EOS Med Chem produce Apalutamide (ARN-509) 956104-40-8 in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok

Apalutamide (ARN-509) , we are China TOP supplier

Name: Apalutamide (ARN-509)

CAS#: 956104-40-8

Chemical Formula: C21H15F4N5O2S

Exact Mass: 477.08826

Molecular Weight: 477.43

Elemental Analysis: C, 52.83; H, 3.17; F, 15.92; N, 14.67; O, 6.70; S, 6.72

EOS Med Chem produce Apalutamide (ARN-509) 956104-40-8 in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.

Apalutamide (ARN-509) 956104-40-8 Intermediates, EOS Med Chem have 8; Apalutamide (ARN-509) 956104-40-8 Impurity we have 10, all from GMP, FDA plant.

Now Apalutamide (ARN-509) 956104-40-8 DMF document is preparing.

Until 2016, Aug, Apalutamide (ARN-509) 956104-40-8 more than produced 25kg API, 120kg Intermediates

Apalutamide (ARN-509) 956104-40-8

Apalutamide (ARN-509) Intermediate 573762-62-6 5-AMINO-3-(TRIFLUOROMETHYL)PICOLINONITRILE

Apalutamide (ARN-509) Intermediate 573762-57-9 5-Nitro-3-trifluoroMethylpyridine-2-carbonitrile

Description: Apalutamide, also known as ARN-509 and JNJ-56021927 , is an androgen receptor antagonist with potential antineoplastic activity. ARN-509 binds to AR in target tissues thereby preventing androgen-induced receptor activation and facilitating the formation of inactive complexes that cannot be translocated to the nucleus. This prevents binding to and transcription of AR-responsive genes. This ultimately inhibits the expression of genes that regulate prostate cancer cell proliferation and may lead to an inhibition of cell growth in AR-expressing tumor cells.

Synonym: ARN509; ARN 509; ARN-509; JNJ56021927; JNJ-56021927; JNJ 56021927; Apalutamide

IUPAC/Chemical Name: 4-(7-(6-cyano-5-(trifluoromethyl)pyridin-3-yl)-8-oxo-6-thioxo-5,7-diazaspiro[3.4]octan-5-yl)-2-fluoro-N-methylbenzamide

SMILES Code: O=C(NC)C1=CC=C(N(C(N(C2=CC(C(F)(F)F)=C(C#N)N=C2)C3=O)=S)C43CCC4)C=C1F

The chemical structure of ARN-509 is very similar structure to  that of Enzalutamide (MDV3100) with two minor modifications: (a) two methyl groups in the 5-member ring of MDV3100 is linked by a CH2 group in ARN-509; (b) the carbon atom in the benzene ring of MDV3100 is replaced by a nitrogen atom in ARN-509. ARN-509 is considered as a Me-Too drug of Enzalutamide (MDV3100). ARN-509 was claimed to be more active than Enzalutamide (MDV3100).

   

ARN-509 is a novel 2nd Generation anti-androgen that is targeted to treat castration resistant prostate cancers where 1st generation anti-androgens fail.  ARN-509 is unique in its action in that it inhibits both AR nuclear translocation and AR binding to androgen response elements in DNA. Importantly, and in contrast to the first-generation anti-androgen bicalutamide, it exhibits no agonist activity in prostate cancer cells that over-express AR. ARN-509 is easily synthesized, and its oral bioavailability and long half-life allow for once-daily oral dosing. In addition, its excellent preclinical safety profile makes it well suited as either a mono- or a combination therapy across the entire spectrum of prostate cancer disease states. (source: http://www.aragonpharm.com/programs/arn509.htm).

   

ARN-509 is  a competitive AR inhibitor, which is fully antagonistic to AR overexpression, a common and important feature of CRPC. ARN-509 was optimized for inhibition of AR transcriptional activity and prostate cancer cell proliferation, pharmacokinetics and in vivo efficacy. In contrast to bicalutamide, ARN-509 lacked significant agonist activity in preclinical models of CRPC. Moreover, ARN-509 lacked inducing activity for AR nuclear localization or DNA binding. In a clinically valid murine xenograft model of human CRPC, ARN-509 showed greater efficacy than MDV3100. Maximal therapeutic response in this model was achieved at 30 mg/kg/day of ARN-509 , whereas the same response required 100 mg/kg/day of MDV3100 and higher steady-state plasma concentrations. Thus, ARN-509 exhibits characteristics predicting a higher therapeutic index with a greater potential to reach maximally efficacious doses in man than current AR antagonists. Our findings offer preclinical proof of principle for ARN-509 as a promising therapeutic in both castration-sensitive and castration-resistant forms of prostate cancer. (source: Cancer Res. 2012 Jan 20. [Epub ahead of print] )

(source: Cancer Res. 2012 Jan 20. [Epub ahead of print] )

1: Clegg NJ, Wongvipat J, Tran C, Ouk S, Dilhas A, Joseph J, Chen Y, Grillot K, Bischoff ED, Cai L, Aparicio A, Dorow S, Arora V, Shao G, Qian J, Zhao H, Yang G, Cao C, Sensintaffar J, Wasielewska T, Herbert MR, Bonnefous C, Darimont B, Scher  HI, Smith-Jones PM, Klang M, Smith ND, de Stanchina E, Wu N, Ouerfelli O, Rix P, Heyman R, Jung ME, Sawyers CL, Hager JH. ARN-509: a novel anti-androgen for prostate cancer treatment. Cancer Res. 2012 Mar 15;72(6):1494-1503. Epub 2012 Jan 20.PubMed  PMID: 22266222.

EOS Med Chem produce Ruxolitinib INCB018424 1092939-17-7 941678-49-5 in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok

Name: Ruxolitinib free base

CAS#: 941678-49-5 (free base)

Chemical Formula: C17H18N6

Exact Mass: 306.15929

Molecular Weight: 306.37

Elemental Analysis: C, 66.65; H, 5.92; N, 27.43

Related CAS#

941678-49-5 (Ruxolitinib free base),

1092939-17-7 (Ruxolitinib phosphate salt).

EOS Med Chem produce Ruxolitinib INCB018424 1092939-17-7  941678-49-5 in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.

Ruxolitinib INCB018424 1092939-17-7  941678-49-5 Intermediates, EOS Med Chem have 8; Ruxolitinib INCB018424 1092939-17-7  941678-49-5 Impurity we have 10, all from GMP, FDA plant.

Now Ruxolitinib INCB018424 1092939-17-7  941678-49-5 DMF document is preparing.

Until 2016, Aug, Ruxolitinib INCB018424 1092939-17-7  941678-49-5 more than produced 25kg API, 120kg Intermediates

Ruxolitinib Intermediates 1146629-84-6 (R)-3-cyclopentyl-3-(4-(4,4,5,5-tetraMethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazol-1-yl)propanenitrile Assay more than 98%, HPLC, NMR, MS is ok

Ruxolitinib Intermediates 1153949-38-2 3-Cyclopentyl-3-[4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazol-1-yl]propanenitrile Assay more than 98%, HPLC, NMR, MS is ok

Ruxolitinib Intermediates 3680-69-1 4-Chloropyrrolo[2,3-d]pyrimidine Assay more than 98%, HPLC, NMR, MS is ok

Ruxolitinib Intermediates 16372-08-0 4-chloro-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidine Assay more than 98%, HPLC, NMR, MS is ok

Ruxolitinib Intermediates 269410-08-4 Pyrazole-4-boronic acid pinacol ester Assay more than 98%, HPLC, NMR, MS is ok

Ruxolitinib Intermediates 591769-05-0 3-CYCLOPENTYLACRYLONITRILE Assay more than 98%, HPLC, NMR, MS is ok

Ruxolitinib Intermediates 941685-27-4 4-(1H-PYRAZOL-4-YL)-7-((2-(TRIMETHYLSILYL)ETHOXY)METHYL)-7H-PYRROLO[2,3-D]PYRIMIDINE Assay more than 98%, HPLC, NMR, MS is ok

Ruxolitinib Intermediates 479633-63-1 4-CHLORO-7-TOSYL-7H-PYRROLO[2,3-D]PYRIMIDINE Assay more than 98%, HPLC, NMR, MS is ok

1: Santos FP, Verstovsek S. Efficacy of ruxolitinib for myelofibrosis. Expert Opin Pharmacother. 2014 Jul;15(10):1465-73. doi: 10.1517/14656566.2014.923404. Epub 2014 May 24. Review. PubMed PMID: 24856675.

2: Molica M, Serrao A, Saracino R, Zacheo I, Stingone C, Alimena G, Breccia M. Disappearance of fibrosis in secondary myelofibrosis after ruxolitinib treatment: new endpoint to achieve? Ann Hematol. 2014 Nov;93(11):1951-2. doi: 10.1007/s00277-014-2096-y. Epub 2014 May 7. Review. PubMed PMID: 24801017.

3: Becker H, Engelhardt M, von Bubnoff N, Wäsch R. Ruxolitinib. Recent Results Cancer Res. 2014;201:249-57. doi: 10.1007/978-3-642-54490-3_16. Review. PubMed PMID: 24756798.

4: Swaim SJ. Ruxolitinib for the treatment of primary myelofibrosis. Am J Health Syst Pharm. 2014 Mar 15;71(6):453-62. doi: 10.2146/ajhp120602. Review. PubMed PMID: 24589536.

5: Mesa RA, Cortes J. Optimizing management of ruxolitinib in patients with myelofibrosis: the need for individualized dosing. J Hematol Oncol. 2013 Oct 22;6:79. doi: 10.1186/1756-8722-6-79. Review. PubMed PMID: 24283870; PubMed Central PMCID: PMC4222119.

6: Kantarjian HM, Silver RT, Komrokji RS, Mesa RA, Tacke R, Harrison CN. Ruxolitinib for myelofibrosis--an update of its clinical effects. Clin Lymphoma Myeloma Leuk. 2013 Dec;13(6):638-45. doi: 10.1016/j.clml.2013.09.006. Epub 2013 Oct 2. Review. PubMed PMID: 24238036.

7: Harrison C, Mesa R, Ross D, Mead A, Keohane C, Gotlib J, Verstovsek S. Practical management of patients with myelofibrosis receiving ruxolitinib. Expert Rev Hematol. 2013 Oct;6(5):511-23. doi: 10.1586/17474086.2013.827413. Epub 2013 Oct 2. Review. PubMed PMID: 24083419.

8: Wade R, Rose M, Neilson AR, Stirk L, Rodriguez-Lopez R, Bowen D, Craig D, Woolacott N. Ruxolitinib for the treatment of myelofibrosis: a NICE single technology appraisal. Pharmacoeconomics. 2013 Oct;31(10):841-52. doi: 10.1007/s40273-013-0083-0. Review. PubMed PMID: 23996108.

9: Lemal R, Robin M, Ravinet A, Cacheux V, Guièze R, Bay JO. [Ruxolitinib prescription in myelofibrosis]. Bull Cancer. 2013 Sep;100(9):897-902. doi: 10.1684/bdc.2013.1792. Review. French. PubMed PMID: 23985569.

10: Kremyanskaya M, Atallah EL, Hoffman R, Mascarenhas JO. Clarifying the use of ruxolitinib in patients with myelofibrosis. Oncology (Williston Park). 2013 Jul;27(7):706-14. Review. Erratum in: Oncology (Williston Park). 2013 Aug;27(8):737. PubMed PMID: 23977767.

11: Mascarenhas J, Hoffman R. A comprehensive review and analysis of the effect of ruxolitinib therapy on the survival of patients with myelofibrosis. Blood. 2013 Jun 13;121(24):4832-7. doi: 10.1182/blood-2013-02-482232. Epub 2013 Apr 9. Review. PubMed PMID: 23570800.

12: Verstovsek S. Ruxolitinib: an oral Janus kinase 1 and Janus kinase 2 inhibitor in the management of myelofibrosis. Postgrad Med. 2013 Jan;125(1):128-35. doi: 10.3810/pgm.2013.01.2628. Review. PubMed PMID: 23391678.

13: Ganetsky A. Ruxolitinib: a new treatment option for myelofibrosis. Pharmacotherapy. 2013 Jan;33(1):84-92. doi: 10.1002/phar.1165. Review. PubMed PMID: 23307549.

14: Vaddi K, Sarlis NJ, Gupta V. Ruxolitinib, an oral JAK1 and JAK2 inhibitor, in myelofibrosis. Expert Opin Pharmacother. 2012 Nov;13(16):2397-407. doi: 10.1517/14656566.2012.732998. Epub 2012 Oct 10. Review. PubMed PMID: 23051187.

15: Mascarenhas J, Mughal TI, Verstovsek S. Biology and clinical management of myeloproliferative neoplasms and development of the JAK inhibitor ruxolitinib. Curr Med Chem. 2012;19(26):4399-413. Review. PubMed PMID: 22830345; PubMed Central PMCID: PMC3480698.

16: Ruxolitinib (Jakafi) for myelofibrosis. Med Lett Drugs Ther. 2012 Apr 2;54(1387):27-8. Review. PubMed PMID: 22469651.

17: Ostojic A, Vrhovac R, Verstovsek S. Ruxolitinib for the treatment of myelofibrosis. Drugs Today (Barc). 2011 Nov;47(11):817-27. doi: 10.1358/dot.2011.47.11.1708829. Review. PubMed PMID: 22146225.

18: Naqvi K, Verstovsek S, Kantarjian H, Ravandi F. A potential role of ruxolitinib in leukemia. Expert Opin Investig Drugs. 2011 Aug;20(8):1159-66. doi: 10.1517/13543784.2011.589383. Epub 2011 Jun 3. Review. PubMed PMID: 21635221; PubMed Central PMCID: PMC4143907.

2016 EOS Med Chem New small molecule and inhibitor

CAS Purity Target Name
91396-88-2 white solid, HPLC more than 98%, NMR,MS is ok stearoyl-coA desaturase 1 (SCD1) NSC 14613, PluriSln 1
1056634-68-4 light yellow solid,  HPLC more than 98%, NMR,MS is ok JAK1/JAK2  Cyt387
188116-07-6 white solid, HPLC more than 98%, NMR,MS is ok GABA AWD 131-138
702675-74-9 white solid, HPLC more than 98%, NMR,MS is ok TBK1， PDK1 BX795
638156-11-3 white solid, HPLC more than 98%, NMR,MS is ok PKD1 CID-2011756
1227633-49-9 white solid, HPLC more than 98%, NMR,MS is ok AhR SetmEegenin 1
1342278-01-6 white solid, HPLC more than 98%, NMR,MS is ok ROCK1， ROCK2 RKI-1447
168682-53-9 white solid, HPLC more than 98%, NMR,MS is ok P1-1 Ezatiostat
1228591-30-7 light yellow solid, HPLC more than 98%, NMR,MS is ok RAF TAK-632
1246560-33-7 white solid, HPLC more than 98%, NMR,MS is ok PI3K， mTOR VS-5584
1011301-27-1 yellow solid, HPLC more than 98%, NMR,MS is ok MDM-2, p53  Tenovin-3
380315-80-0 white solid, HPLC more than 98%, NMR,MS is ok SIRT1， SIRT2  Tenovin-1
1011557-82-6 yellow solid, HPLC more than 98%, NMR,MS is ok, HCl salt SIRT1， SIRT2 Tenovin-6
931398-72-0 white solid, HPLC more than 98%, NMR,MS is ok PHD   IOX2
213261-59-7 yellow solid, HPLC more than 98%, NMR,MS is ok p53 RITA
778270-11-4 white solid, HPLC more than 98%, NMR,MS is ok Bcr-Abl GNF-2
5142-23-4 white solid, HPLC more than 98%, NMR,MS is ok PI3K  NSC 66389,3-MA
154235-83-3 light yellow solid,  HPLC more than 98%, NMR,MS is ok AMPA  Ampalex ，CX-516
"905973-89-9
" light yellow solid,  HPLC more than 98%, NMR,MS is ok "ATM/ATR CGK 733
"
487021-52-3 brown solid,HPLC more than 98%, NMR,MS is ok GSK3β AR-A014418
881202-45-5 brown solid,HPLC more than 98%, NMR,MS is ok HDM2  JNJ26854165
414864-00-9 white solid, HPLC more than 98%, NMR,MS is ok HDAC PXD101, Beliomstat
442-52-4 light yellow solid, HPLC more than 98%, NMR,MS is ok Histamine Receptor Clemizole
371242-69-2 light yellow solid,  HPLC more than 98%, NMR,MS is ok PI3K IC-87114
476-34-6 red solid, HPLC more than 98%, NMR,MS is ok isoindigotin
483367-10-8 white solid, HPLC more than 98%, NMR,MS is ok Smo Purmorphamine
870281-82-6 white solid, HPLC more than 98%, NMR,MS is ok PI3K CAL-101
112522-64-2 white solid, HPLC more than 98%, NMR,MS is ok HDAC1 CI-994
1125780-41-7 white solid, HPLC more than 98%, NMR,MS is ok VEGFR SKLB 610
656820-32-5 white solid, HPLC more than 98%, NMR,MS is ok human A3 adenosine receptor Reversine
304448-55-3 light yellow solid,  HPLC more than 98%, NMR,MS is ok dynamin Dynasore
XL019,945755-56-6 light yellow solid,  HPLC more than 98%, NMR,MS is ok JAK2 XL019, 945755-56-6
152121-53-4 yellow solid, HPLC more than 98%, NMR,MS is ok p38 MAPK  PD 169316
1342276-76-9 white solid, HPLC more than 98%, NMR,MS is ok ROCK1， ROCK2 RKI-1313
1246535-95-4 white solid, HPLC more than 98%, NMR,MS is ok 1246535-95-4
1033836-12-2, white solid, HPLC more than 98%, NMR,MS is ok HPGDS HPGDS-inhibitor-1
130798-51-5 white solid, HPLC more than 98%, NMR,MS is ok NMDA MDL 29951
1033769-28-6 red solid, 98 Trk GNF 5837
587841-73-4 white solid, HPLC more than 98%, NMR,MS is ok Cdc42 ZCL 278
929016-96-6 white solid, HPLC more than 98%, NMR,MS is ok HDAC SB 939
452342-67-5 white solid, HPLC more than 98%, NMR,MS is ok ALK5 GW788388
162640-98-4 white solid, HPLC more than 98%, NMR,MS is ok AT-56
1418013-75-8 white solid, HPLC more than 98%, NMR,MS is ok VCP/p97 1418013-75-8
423735-93-7 white solid, HPLC more than 98%, NMR,MS is ok PAR1 ML 161
664993-53-7 white solid, HPLC more than 98%, NMR,MS is ok PARP JW55
"944396-07-0
" white solid, HPLC more than 98%, NMR,MS is ok PI3K NVP-BKM120, Buparlisib
30544-47-9 light yellow oil, HPLC more than 98%, NMR,MS is ok Others Etofenamate
1197300-24-5 white solid, HPLC more than 98%, NMR,MS is ok TGR5(GPCR19) TGR5
1270138-40-3 white solid, HPLC more than 98%, NMR,MS is ok Others NSI-189
212844-54-7 white solid,  96.5% CDK Purvalanol B(NG 95)
"1349796-36-6
" light yellow solid, HPLC more than 98%, NMR,MS is ok PI3K， mTOR  XL-765
36945-98-9 light yellow solid, HPLC more than 98%, NMR,MS is ok TRPM8 ICILIN
"1161205-04-4
" white solid, HPLC more than 98%, NMR,MS is ok "PAM  VU 0361737
"
"55778-02-4
" white solid, HPLC more than 98%, NMR,MS is ok "CXCR4  WZ 811
"
"79183-19-0
" yellow solid, HPLC more than 98%, NMR,MS is ok Apoptosis Activator 2 Apoptosis Activator 2
1594094-64-0 white solid, HPLC more than 98%, NMR,MS is ok Kinesin CW069
244767-67-7 white solid, HPLC more than 98%, NMR,MS is ok HIV Dapivirine，TMC-120
224177-60-0 white solid, HPLC more than 98%, NMR,MS is ok , HCl salt sigma-2 Siramesine.HCl
147817-50-3 white solid, HPLC more than 98%, NMR,MS is ok sigma-2 Siramesine
1432660-47-3 white solid, HPLC more than 98%, NMR,MS is ok IDH AGI-6780
878141-96-9 white solid, HPLC more than 98%, NMR,MS is ok, HCl salt sigma-1 S1RA
330942-05-7 light yellow solid, HPLC more than 98%, NMR,MS is ok FXa Betrixaban
442632-72-6 white solid, HPLC more than 98%, NMR,MS is ok Arp2/3 CK-636
309271-94-1 light yellow solid, HPLC more than 98%, NMR,MS is ok SIRT1  Inauhzin
97207-47-1 red solid, HPLC more than 98%, NMR,MS is ok Apoptosis Inducer Methylisoindigotin
354813-19-7 white solid, HPLC more than 98%, NMR,MS is ok Cathepsin Balicatib
878419-78-4 light yellow solid, HPLC more than 98%, NMR,MS is ok Antibacterial Walrycin B
1177827-73-4 white solid, HPLC more than 98%, NMR,MS is ok, HCl salt Enolase AP-III-a4
778277-15-9 white solid, HPLC more than 98%, NMR,MS is ok Bcr-Abl   GNF-5
1192224-24-0 white solid, HPLC more than 98%, NMR,MS is ok Des(benzylpyridyl) Atazanavi
438190-29-5 white solid, HPLC more than 98%, NMR,MS is ok Pim SMI 4a
6501-72-0 white solid, HPLC more than 98%, NMR,MS is ok Others VGX-1027
288250-47-5 white solid, HPLC more than 98%, NMR,MS is ok Interleukin Related  288250-47-5
1469924-27-3 white solid, HPLC more than 98%, NMR,MS is ok ATGL Atglistatin
1005491-05-3 white solid, HPLC more than 98%, NMR,MS is ok others Tirasemtiv(CK-2017357)
64862-96-0 bule solid, >95 Ametantrone(NSC 196473)
436133-68-5 light yellow solid, HPLC more than 98%, NMR,MS is ok Ras Kobe0065
89464-63-1 white solid, HPLC more than 98%, NMR,MS is ok HIF-PH Dimethyloxaloylglycine (DMOG)
301353-96-8 white solid, HPLC more than 98%, NMR,MS is ok NAMPT P7C3
1235481-43-2 white solid, HPLC more than 98%, NMR,MS is ok NAMPT (R)-P7C3-OMe
2076-91-7 white solid, HPLC more than 98%, NMR,MS is ok, (Dihydrochloride) Others TPT-260.2HCl
1202916-90-2 yellow solid, HPLC more than 98%, NMR,MS is ok, HCl salt Pim  CX-6258
931706-15-9 white solid, HPLC more than 98%, NMR,MS is ok CFTR PPQ-102
1226895-20-0 light yellow solid, HPLC more than 98%, NMR,MS is ok ATB 346
775304-57-9 white solid, HPLC more than 98%, NMR,MS is ok CFTR PTC124
4311-88-0 light yellow solid, HPLC more than 98%, NMR,MS is ok RIP1 Necrostatin-1
591778-68-6 light yellow solid, HPLC more than 98%, NMR,MS is ok, HCl salt Others CP 640186
370586-05-3 light yellow solid, HPLC more than 98%, NMR,MS is ok others CID 797718
PR-619,2645-32-1 light yellow solid, HPLC more than 98%, NMR,MS is ok Deubiquitinase PR-619, 2645-32-1
65646-68-6 yellow solid, HPLC more than 98%, NMR,MS is ok RAR/RXR Fenretinide
518058-84-9 white solid, HPLC more than 98%, NMR,MS is ok Src-PTK KX1-004
1421923-86-5 white solid, HPLC more than 98%, NMR,MS is ok KPT-330, (E)-RN
329907-28-0 white solid, HPLC more than 98%, NMR,MS is ok Casein Kinase TTP 22
1415238-77-5 white solid, HPLC more than 98%, NMR,MS is ok others 5S rRNA modificator
173352-21-1 white solid, HPLC more than 98%, NMR,MS is ok, HCl salt others CM 346(Obenoxazine)
1402836-58-1 white solid, HPLC more than 98%, NMR,MS is ok IDO NLG919
2044451 white solid, HPLC more than 98%, NMR,MS is ok MT1-MMP NSC 405020
67469-81-2 white solid, HPLC more than 98%, NMR,MS is ok, (dihydrochloride) Dopamine Reuptake Inhibitor GBR 12935
1515856-92-4 white solid, HPLC more than 98%, NMR,MS is ok, HCl salt endothelial lipase  XEN445
1395084-25-9 red solid, HPLC more than 98%, NMR,MS is ok BRD4 MS436
1314890-29-3 white solid, HPLC more than 98%, NMR,MS is ok HDAC1 TMP269
1350622-33-1 white solid, HPLC more than 98%, NMR,MS is ok kb-NB77-78
1403783-31-2 white solid, HPLC more than 98%, NMR,MS is ok Nexturastat A
639052-78-1 white solid, HPLC more than 98%, NMR,MS is ok LH846
195371-52-9 light yellow oil, HPLC more than 98%, NMR,MS is ok NSC 42834
832714-46-2 white solid, HPLC more than 98%, NMR,MS is ok APD668
950736-05-7 yellow solid, HPLC more than 98%, NMR,MS is ok B-Raf IN 1
Ro61-8048,199666-03-0 light yellow solid, HPLC more than 98%, NMR,MS is ok Ro 61-8048,199666-03-0
837422-57-8 white solid, HPLC more than 98%, NMR,MS is ok WH-4-023
49671-76-3 white solid, HPLC more than 98%, NMR,MS is ok ZLN005
454453-49-7 light yellow solid, HPLC more than 98%, NMR,MS is ok kobe2602
208260-29-1 white solid, HPLC more than 98%, NMR,MS is ok  ZM336372
199596-05-9(E) white solid, HPLC more than 98%, NMR,MS is ok JIB-04 (NSC 693627)
199596-24-2 yellow solid, HPLC more than 98%, NMR,MS is ok Z-JIB-04 (NSC 693627)
1421227-53-3 light yellow solid, HPLC more than 98%, NMR,MS is ok  WS6
1421227-52-2 light yellow solid, HPLC more than 98%, NMR,MS is ok  WS3
6506-37-2 light yellow solid, HPLC more than 98%, NMR,MS is ok Nimorazole
1026680-07-8 white solid, HPLC more than 98%, NMR,MS is ok  LB-100
338967-87-6 light yellow solid, HPLC more than 98%, NMR,MS is ok Mdivi-1
6497-78-5 light yellow solid, HPLC more than 98%, NMR,MS is ok RGW 611
548470-11-7 white solid, HPLC more than 98%, NMR,MS is ok ISRIB
1163-36-6 white solid, HPLC more than 98%, NMR,MS is ok Clemizole.HCl
1443139-14-7 white solid, HPLC more than 98%, NMR,MS is ok GSK124576A
1009734-33-1 white solid, HPLC more than 98%, NMR,MS is ok 1009734-33-1
396129-53-6 light yellow solid, HPLC more than 98%, NMR,MS is ok LY-364947
79455-30-4 white solid, HPLC more than 98%, NMR,MS is ok Nicaraven
1350920-22-7 white solid, HPLC more than 98%, NMR,MS is ok T.cruzi Inhibitor
1420071-30-2 yellow solid, HPLC more than 98%, NMR,MS is ok% Bioymifi
1019331-10-2 white solid, HPLC more than 98%, NMR,MS is ok S0859
743420-02-2 white solid, HPLC more than 98%, NMR,MS is ok Chidamide
1146963-51-0 light yellow solid,HPLC more than 98%, NMR,MS is ok% J147
118409-57-7 light yellow solid,HPLC more than 98%, NMR,MS is ok% AG18
1233948-35-0 yellow solid,HPLC more than 98%, NMR,MS is ok% ELR-510444
285986-88-1 white solid, HPLC more than 98%, NMR,MS is ok% CCG1423
48208-26-0 light yellow solid, HPLC more than 98%, NMR,MS is ok% RG108
72702-95-5 white solid, HPLC more than 98%, NMR,MS is ok% STATIL
218156-96-8 light yellow solid, HPLC more than 98%, NMR,MS is ok% SRPIN 340
1118807-13-8 light yellow solid, HPLC more than 98%, NMR,MS is ok% KY02111
1439934-41-4 off white solid, HPLC more than 98%, NMR,MS is ok% CTx0294885
761437-28-9 light yellow solid, HPLC more than 98%, NMR,MS is ok% TAE-226
1430089-64-7 off white solid, HPLC more than 98%, NMR,MS is ok% UNC0064-12
4727-31-5 off white solid, HPLC more than 98%, NMR,MS is ok%  Kartogenin
1262618-39-2 white solid, HPLC more than 98%, NMR,MS is ok% GS967
83797-69-7 light yellow solid, HPLC more than 98%, NMR,MS is ok% GTPL5846
393105-53-8 light yellow solid, HPLC more than 98%, NMR,MS is ok% Tiplaxtinin(PAI-039)
326914-06-1 light yellow solid, HPLC more than 98%, NMR,MS is ok% MHY1485
212844-53-6 white solid, HPLC more than 98%, NMR,MS is ok% PURVALANOL A
212779-48-1 white solid, HPLC more than 98%, NMR,MS is ok% NG-52
202475-60-3 light yellow solid, HPLC more than 98%, NMR,MS is ok% WHI-P131
211555-08-7 white solid, HPLC more than 98%, NMR,MS is ok% WHI-P180
153436-53-4 white solid, HPLC more than 98%, NMR,MS is ok% AG-1478
153436-54-5 white solid, HPLC more than 98%, NMR,MS is ok% AG-1517
189290-58-2 white solid, HPLC more than 98%, NMR,MS is ok% AG-1557
189232-42-6 white solid, HPLC more than 98%, NMR,MS is ok% Bohemine
186692-46-6 white solid, HPLC more than 98%, NMR,MS is ok% Roscovitine
21561-09-1 white solid, HPLC more than 98%, NMR,MS is ok% WHI-P258
65162-13-2 red solid, 98% 1-Methoxy PMS
1191911-27-9 white solid, HPLC more than 98%, NMR,MS is ok% CZC-54252
951650-22-9 white solid, HPLC more than 98%, NMR,MS is ok% NS 11394
1233533-04-4 white solid, HPLC more than 98%, NMR,MS is ok% kb NB 142-70
1232221-74-7 light yellow solid, HPLC more than 98%, NMR,MS is ok% APY0201
951654-29-8 white solid, HPLC more than 98%, NMR,MS is ok% 951654-29-8
540769-28-6 white solid, HPLC more than 98%, NMR,MS is ok% ACT 058362; Palosuran
425399-05-9 light yellow solid, HPLC more than 98%, NMR,MS is ok%  Casin
1345847-93-9 white solid, HPLC more than 98%, NMR,MS is ok% Altiratinib
574013-66-4 yellow solid, HPLC more than 98%, NMR,MS is ok% fexaramine
71320-77-9 white solid, HPLC more than 98%, NMR,MS is ok% Moclobemide
851881-60-2 white solid, HPLC more than 98%, NMR,MS is ok% ADX 47273
1094042-01-9 light yellow solid, HPLC more than 98%, NMR,MS is ok% CYM5442
1527473-33-1 off white solid,HPLC more than 98%, NMR,MS is ok% PF-06447475
950769-58-1 light yellow solid, HPLC more than 98%, NMR,MS is ok% Quizartinib, AC-220
376640-41-4 white solid, HPLC more than 98%, NMR,MS is ok% BVT 2733
516480-79-8 white solid, HPLC more than 98%, NMR,MS is ok% BML-277
944261-79-4 white solid, HPLC more than 98%, NMR,MS is ok% A-803467
6310-41-4 white solid, HPLC more than 98%, NMR,MS is ok% NSC-41589
1370256-78-2 white solid, HPLC more than 98%, NMR,MS is ok% FLT3-IN-1
852475-26-4 yellow solid, HPLC more than 98%, NMR,MS is ok% MC1568
1609960-30-6 white solid, HPLC more than 98%, NMR,MS is ok% TH287
204005-46-9 light yellow solid,  HPLC more than 98%, NMR,MS is ok Semaxinib(SU 5416)
1609960-31-7 white solid, HPLC more than 98%, NMR,MS is ok% TH588
178606-66-1 white solid, HPLC more than 98%, NMR,MS is ok% U-104
300586-90-7 light yellow solid, HPLC more than 98%, NMR,MS is ok% OAC1
6019-39-2 light yellow solid, HPLC more than 98%, NMR,MS is ok% OAC2
104821-25-2 red solid, HPLC more than 98%, NMR,MS is ok% Dihydroethidium
541550-19-0 white solid, HPLC more than 98%, NMR,MS is ok% Apilimod
870087-36-8 white solid, HPLC more than 98%, NMR,MS is ok% Apilimod mesylate
172732-68-2 white solid, HPLC more than 98%, NMR,MS is ok% varespladib , LY315920
587850-67-7 white solid, HPLC more than 98%, NMR,MS is ok% C7280948
778274-97-8 white solid, HPLC more than 98%, NMR,MS is ok% Multi-kinase inhibitor I
185298-58-2 white solid, HPLC more than 98%, NMR,MS is ok% 185298-58-2
896705-16-1 light yellow solid, HPLC more than 98%, NMR,MS is ok% BMH-21
1327167-19-0 white solid, HPLC more than 98%, NMR,MS is ok% BPR1J-097
70806-55-2 white solid, HPLC more than 98%, NMR,MS is ok% trans-Tranilast
1225037-39-7 white solid, HPLC more than 98%, NMR,MS is ok% PQR-309
173903-47-4 light yellow solid, HPLC more than 98%, NMR,MS is ok% Tizoxanide
1477949-42-0 white solid, HPLC more than 98%, NMR,MS is ok% CAY10683 (SantacruzaMate A)
1637739-82-2 white solid, HPLC more than 98%, NMR,MS is ok% BQU57
318290-98-1 light yellow  oil, HPLC more than 98%, NMR,MS is ok% Fluensulfone
138847-85-5 white solid, HPLC more than 98%, NMR,MS is ok% PRE 084.HCl
66592-89-0 white solid, HPLC more than 98%, NMR,MS is ok% KEVETRIN
603148-36-3 light yellow solid, HPLC more than 98%, NMR,MS is ok% Azeliragon
312917-14-9 light yellow solid, HPLC more than 98%, NMR,MS is ok% SC-202671
219911-35-0 light yellow solid, HPLC more than 98%, NMR,MS is ok% MPEP hydrochloride
925701-49-1 light yellow solid, HPLC more than 98%, NMR,MS is ok%  KU-60019
1619994-68-1 light yellow solid, HPLC more than 98%, NMR,MS is ok% GSK2801
165682-93-9 light yellow solid, HPLC more than 98%, NMR,MS is ok% O4I2
1016535-83-3 light yellow solid, HPLC more than 98%, NMR,MS is ok% Oct3 and 4-inducer-1
175135-47-4 light yellow solid, HPLC more than 98%, NMR,MS is ok% O4I1
1235481-90-9 light yellow solid, HPLC more than 98%, NMR,MS is ok% P7C3-A20
220904-99-4 red solid, HPLC more than 98%, NMR,MS is ok% 220904-99-4
10537-47-0 light yellow solid, HPLC more than 98%, NMR,MS is ok% Tyrphostin 9
1415716-58-3 white solid, HPLC more than 98%, NMR,MS is ok% TG6-10-1
635324-72-0 white solid, HPLC more than 98%, NMR,MS is ok% CTLA-4 - inhibitor
71748-57-7 light yellow solid, HPLC more than 98%, NMR,MS is ok% 4-Keto 13-cis-Retinoic Acid
910232-84-7 white solid, HPLC more than 98%, NMR,MS is ok% CGI-1746
671225-39-1 white solid, HPLC more than 98%, NMR,MS is ok% Cardiogenol C HCl
200484-11-3 white solid, HPLC more than 98%, NMR,MS is ok% CHS 828
1094873-14-9 white solid, HPLC more than 98%, NMR,MS is ok% JNJ 31020028
873697-71-3 white solid, HPLC more than 98%, NMR,MS is ok% CK 1827452
1223001-51-1 light yellow solid, HPLC more than 98%, NMR,MS is ok% Torin 2
188011-69-0 white solid, HPLC more than 98%, NMR,MS is ok% Bikinin
537034-17-6 white solid, HPLC more than 98%, NMR,MS is ok% BML210
937039-45-7 white solid, HPLC more than 98%, NMR,MS is ok% TC-H 106
504433-23-2 light yellow solid,HPLC more than 98%, NMR,MS is ok% GW441756
537672-41-6 white solid, HPLC more than 98%, NMR,MS is ok% UF 010
601514-19-6 light yellow solid, HPLC more than 98%, NMR,MS is ok% TWS119
927822-86-4 white solid, HPLC more than 98%, NMR,MS is ok% KC7F2
890190-22-4 light yellow solid, HPLC more than 98%, NMR,MS is ok% WDR5 0103
92831-11-3 white solid, HPLC more than 98%, NMR,MS is ok% MN 64
848354-66-5 white solid, HPLC more than 98%, NMR,MS is ok% NCH 51
5638-76-6 light yellow oil, HPLC more than 98%, NMR,MS is ok% Betahistine
5452-87-9 light yellow oil, HPLC more than 98%, NMR,MS is ok% NSC19005
537034-15-4 white solid, HPLC more than 98%, NMR,MS is ok% NKL 22
1222998-36-8 light yellow solid, HPLC more than 98%, NMR,MS is ok% Torin-1
929007-72-7 light yellow solid, HPLC more than 98%, NMR,MS is ok% DB07268
522650-83-5 light yellow solid, HPLC more than 98%, NMR,MS is ok% SW-044248
361185-42-4 light yellow solid, HPLC more than 98%, NMR,MS is ok% RBC8
718635-93-9 light yellow solid, HPLC more than 98%, NMR,MS is ok% TETRABENAZINE
1208319-26-9 white solid, HPLC more than 98%, NMR,MS is ok% PF03394197
38136-70-8 white solid, HPLC more than 98%, NMR,MS is ok% Brevianamide F
960539-70-2 white solid, HPLC more than 98%, NMR,MS is ok% GSK1278863
199986-75-9 white solid, HPLC more than 98%, NMR,MS is ok% CVT-313
736994-63-1 off white solid, HPLC more than 98%, NMR,MS is ok% Cyantraniliprole
PF-CBP1 light yellow solid, HPLC more than 98%, NMR,MS is ok%, HCl salt PF-CBP1
448895-37-2 white solid, HPLC more than 98%, NMR,MS is ok% NS1643
839706-07-9 white solid, HPLC more than 98%, NMR,MS is ok% GNF-7
,1346528-06-0 white solid, HPLC more than 98%, NMR,MS is ok% ML241.HCl
371934-59-7 light yellow solid, HPLC more than 98%, NMR,MS is ok% PIK-inhibitors
865783-99-9 white solid, HPLC more than 98%, NMR,MS is ok% Briciclib
55142-85-3 light yellow oil, HPLC more than 98%, NMR,MS is ok% Ticlopidine
53885-35-1 white solid, HPLC more than 98%, NMR,MS is ok% Ticlopidine.HCl
371942-69-7 light yellow solid, HPLC more than 98%, NMR,MS is ok% YM-201636
1346527-98-7 light yellow solid, HPLC more than 98%, NMR,MS is ok% ML240
312636-16-1 white solid, HPLC more than 98%, NMR,MS is ok% SKI II (SphK-I2)
(S)-5-(3-(heptyloxy)-5-(octan-2-yloxy)benzyloxy)isophthalicacid white solid, HPLC more than 98%, NMR,MS is ok% (S)-5-(3-(heptyloxy)-5-(octan-2-yloxy)benzyloxy)isophthalic acid
(R)-5-(3-(heptyloxy)-5-(octan-2-yloxy)benzyloxy)isophthalicacid white solid, HPLC more than 98%, NMR,MS is ok% (R)-5-(3-(heptyloxy)-5-(octan-2-yloxy)benzyloxy)isophthalic acid
5-(3-((R)-octan-2-yloxy)-5-((S)-octan-2-yloxy)benzyloxy)isophthalicacid white solid, HPLC more than 98%, NMR,MS is ok% 5-(3-((R)-octan-2-yloxy)-5-((S)-octan-2-yloxy)benzyloxy)isophthalic acid
5-(3,5-bis((S)-octan-2-yloxy)benzyloxy)isophthalicacid white solid, HPLC more than 98%, NMR,MS is ok% 5-(3,5-bis((S)-octan-2-yloxy)benzyloxy)isophthalic acid
5-(3,5-bis((R)-octan-2-yloxy)benzyloxy)isophthalicacid white solid, HPLC more than 98%, NMR,MS is ok% 5-(3,5-bis((R)-octan-2-yloxy)benzyloxy)isophthalic acid
5-(3-(heptan-2-yloxy)-5-(hexyloxy)benzyloxy)isophthalicacid white solid, HPLC more than 98%, NMR,MS is ok% 5-(3-(heptan-2-yloxy)-5-(hexyloxy)benzyloxy)isophthalic acid
5-(3,5-bis(heptan-2-yloxy)benzyloxy)isophthalicacid white solid, HPLC more than 98%, NMR,MS is ok% 5-(3,5-bis(heptan-2-yloxy)benzyloxy)isophthalic acid
18274-81-2 yellow solid, HPLC more than 98%, NMR,MS is ok% Desmethylanethol trithione
1454585-06-8 white solid, HPLC more than 98%, NMR,MS is ok% SR-3029
919351-41-0 white solid, HPLC more than 98%, NMR,MS is ok% AZD1283
186611-52-9 yellow solid,HPLC more than 98%, NMR,MS is ok% IC261
183619-38-7 white solid, HPLC more than 98%, NMR,MS is ok% CPI-1189
92262-58-3 white solid, HPLC more than 98%, NMR,MS is ok% Valrocemide
82351-05-1 white solid, HPLC more than 98%, NMR,MS is ok% Lvguidingan
1346547-00-9 light yellow solid, HPLC more than 98%, NMR,MS is ok% GSK583
310456-65-6 yellow solid, HPLC more than 98%, NMR,MS is ok% IMR-1
1445605-23-1 white solid, HPLC more than 98%, NMR,MS is ok% Lu AF21934
1093757-42-6 light brown solid,HPLC more than 98%, NMR,MS is ok% UV0155041
175026-96-7 light yellow solid, HPLC more than 98%, NMR,MS is ok% NQDI-1
331862-41-0 yellow solid, HPLC more than 98%, NMR,MS is ok% IMR-1A
1228013-15-7 light brown solid,HPLC more than 98%, NMR,MS is ok% CC-115
1821428-35-6 white solid, HPLC more than 98%, NMR,MS is ok% AZD-0156
 308831-61-0 light yellow solid, HPLC more than 98%, NMR,MS is ok% tak-013
472981-92-3 white solid, HPLC more than 98%, NMR,MS is ok% SB 366791
349085-82-1 white solid, HPLC more than 98%, NMR,MS is ok% GSK137647A
3476-86-6 yellow solid,HPLC more than 98%, NMR,MS is ok% SU 5205
SU4942,76086-99-2 yellow solid,HPLC more than 98%, NMR,MS is ok% SU 4942, 76086-99-2
186611-55-2 yellow solid,HPLC more than 98%, NMR,MS is ok% SU 4313
186611-04-1 yellow solid,HPLC more than 98%, NMR,MS is ok% SU 5214
5812/7/7 red solid,HPLC more than 98%, NMR,MS is ok% NSC 86429
114727-43-4 yellow solid,HPLC more than 98%, NMR,MS is ok% NSC 247030
865536-65-8 yellow solid,HPLC more than 98%, NMR,MS is ok% 4-Oxofenretinide
376638-65-2 light yellow solid, HPLC more than 98%, NMR,MS is ok%, HCl salt BVT-14225
150493-34-8 white solid, HPLC more than 98%, NMR,MS is ok% NS 638
136831-48-6 light yellow solid, HPLC more than 98%, NMR,MS is ok% RG 13022
1025015-40-0 off white solid, HPLC more than 98%, NMR,MS is ok% GK921
885066-67-1 white solid, HPLC more than 98%, NMR,MS is ok% PGD2-inhibitor
77858-21-0 light yellow solid, HPLC more than 98%, NMR,MS is ok% velaresol
918348-67-1 light yellow solid, HPLC more than 98%, NMR,MS is ok% XL-652
51213-99-1 white solid, HPLC more than 98%, NMR,MS is ok% Clanfenur
174262-13-6 white solid, HPLC more than 98%, NMR,MS is ok% SDZ285-428
575474-82-7 off white solid,HPLC more than 98%, NMR,MS is ok% R112
135779-82-7 white solid, HPLC more than 98%, NMR,MS is ok% Bamaquimast
55104-39-7 white solid, HPLC more than 98%, NMR,MS is ok% DL-071-IT
4550-72-5 white solid, HPLC more than 98%, NMR,MS is ok% NSC 15364
KDM5-inhibitor white solid, HPLC more than 98%, NMR,MS is ok% KDM5-inhibitor
52029-86-4 yellow solid, HPLC more than 98%, NMR,MS is ok% STO-609
306-07-0 white solid, HPLC more than 98%, NMR,MS is ok% PARGYLINE HYDROCHLORIDE
1628208-23-0 white solid, HPLC more than 98%, NMR,MS is ok% CPI-455
178946-89-9 white solid, HPLC more than 98%, NMR,MS is ok% C-DIM12
429653-73-6 white solid, HPLC more than 98%, NMR,MS is ok% Y16

EOS Med Chem produce Abemaciclib ( LY2835219) 1231929-97-7 in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.

Name: Abemaciclib ( LY2835219)

CAS#: 1231929-97-7 (free base)

Chemical Formula: C27H32F2N8

Exact Mass: 506.2718

Molecular Weight: 506.59339

Elemental Analysis: C, 64.01; H, 6.37; F, 7.50; N, 22.12

EOS Med Chem produce Abemaciclib ( LY2835219) 1231929-97-7  in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.

Abemaciclib ( LY2835219) 1231929-97-7  Intermediates, EOS Med Chem have 8; Abemaciclib ( LY2835219) 1231929-97-7  Impurity we have 10, all from GMP, FDA plaAnt.

Now Abemaciclib ( LY2835219) 1231929-97-7  DMF document is preparing.

Until 2016, Aug, Abemaciclib ( LY2835219) 1231929-97-7  more than produced 25kg API, 120kg Intermediates

Related CAS#

CAS#1231929-97-7 (LY2835219 free base)

CAS# 1231930-82-7 (LY2835219 mesylate salt).

Abemaciclib ( LY2835219) 1231929-97-7 Abemaciclib ( LY2835219)

Abemaciclib ( LY2835219) Intermediate 67567-26-4, assay 99% in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.

Abemaciclib ( LY2835220) Intermediate 1180132-17-5, assay 99% in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.

Abemaciclib ( LY2835221) Intermediate 1231930-42-9, assay 99% in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.

Abemaciclib ( LY2835222) Intermediate 1231929-97-7, assay 99% in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.

Abemaciclib ( LY2835223) Intermediate 1231930-33-8, assay 99% in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.

Abemaciclib ( LY2835224) Intermediate 1231930-82-7, assay 99% in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.

Description: Abemaciclib, also known as LY2835219, is orally available cyclin-dependent kinase (CDK) inhibitor that targets the CDK4 (cyclin D1) and CDK6 (cyclin D3) cell cycle pathway, with potential antineoplastic activity. LY2835219 inhibits CDK4 and CDK6 with low nanomolar potency. LY2835219 specifically inhibits CDK4 and 6, thereby inhibiting retinoblastoma (Rb) protein phosphorylation in early G1. Inhibition of Rb phosphorylation prevents CDK-mediated G1-S phase transition, thereby arresting the cell cycle in the G1 phase, suppressing DNA synthesis and inhibiting cancer cell growth.

Synonym: LY2835219; LY2835219; LY 2835219; Abemaciclib.

IUPAC/Chemical Name: N-(5-((4-ethylpiperazin-1-yl)methyl)pyridin-2-yl)-5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazol-6-yl)pyrimidin-2-amine

SMILES Code: CC1=NC2=C(F)C=C(C3=NC(NC4=NC=C(CN5CCN(CC)CC5)C=C4)=NC=C3F)C=C2N1C(C)C

1: Yadav V, Burke TF, Huber L, Van Horn RD, Zhang Y, Buchanan SG, Chan EM, Starling JJ, Beckmann RP, Peng SB. The CDK4/6 Inhibitor LY2835219 Overcomes Vemurafenib Resistance Resulting from MAPK Reactivation and Cyclin D1 Upregulation. Mol Cancer Ther. 2014 Aug 13. pii: molcanther.0257.2014. [Epub ahead of print] PubMed PMID: 25122067.

2: Gelbert LM, Cai S, Lin X, Sanchez-Martinez C, Del Prado M, Lallena MJ, Torres R, Ajamie RT, Wishart GN, Flack RS, Neubauer BL, Young J, Chan EM, Iversen P, Cronier D, Kreklau E, de Dios A. Preclinical characterization of the CDK4/6 inhibitor LY2835219: in-vivo cell cycle-dependent/independent anti-tumor activities alone/in combination with gemcitabine. Invest New Drugs. 2014 Jun 13. [Epub ahead of print] PubMed PMID: 24919854.

3: Tate SC, Cai S, Ajamie RT, Burke T, Beckmann RP, Chan EM, De Dios A, Wishart GN, Gelbert LM, Cronier DM. Semi-mechanistic pharmacokinetic/pharmacodynamic modeling of the antitumor activity of LY2835219, a new cyclin-dependent kinase 4/6 inhibitor, in mice bearing human tumor xenografts. Clin Cancer Res. 2014 Jul 15;20(14):3763-74. doi: 10.1158/1078-0432.CCR-13-2846. Epub 2014 May 21. PubMed PMID: 24850847.

4: Dickson MA. Molecular pathways: CDK4 inhibitors for cancer therapy. Clin Cancer Res. 2014 Jul 1;20(13):3379-83. doi: 10.1158/1078-0432.CCR-13-1551. Epub 2014 May 2. PubMed PMID: 24795392.

EOS Med Chem produce Omarigliptin MK3102 1226781-44-7 in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.

Name: Omarigliptin

CAS#: 1226781-44-7

Chemical Formula: C17H20F2N4O3S

Exact Mass: 398.12242

Molecular Weight: 398.43

Elemental Analysis: C, 51.25; H, 5.06; F, 9.54; N, 14.06; O, 12.05; S, 8.05

EOS Med Chem produce Omarigliptin  MK3102  1226781-44-7 in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.

Omarigliptin  MK3102  1226781-44-7 Intermediates, EOS Med Chem have 8; Omarigliptin  MK3102  1226781-44-7 Impurity we have 10, all from GMP, FDA plant.

Now Omarigliptin  MK3102  1226781-44-7 DMF document is preparing.

Until 2016, Aug, Omarigliptin  MK3102  1226781-44-7 more than produced 25kg API, 120kg Intermediates

omarigliptin Intermediate N-[(2R,3S)-2-(2,5-difluorophenyl)tetrahydro-5-oxo-2H-pyran-3-yl]-CarbaMic acid 1,1-diMethylethyl ester 951127-25-6

omarigliptin Intermediate 2-(Methylsulfonyl)-2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole 1280210-80-1

Description: Omarigliptin, also known as MK-3102, is a potent and long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes. MK-3102 (omarigliptin), was identified as a potent and selective dipeptidyl peptidase 4 (DPP-4) inhibitor with an excellent pharmacokinetic profile amenable for once-weekly human dosing and selected as a clinical development candidate. Omarigliptin is currently in phase 3 clinical development.

Synonym: MK3102; MK-3102; MK 3102; Omarigliptin

IUPAC/Chemical Name: (2R,3S,5R)-2-(2,5-difluorophenyl)-5-(2-(methylsulfonyl)pyrrolo[3,4-c]pyrazol-5(2H,4H,6H)-yl)tetrahydro-2H-pyran-3-amine

SMILES Code: N[C@@H]1[C@@H](C2=CC(F)=CC=C2F)OC[C@H](N3CC4=NN(S(=O)(C)=O)C=C4C3)C1

1: Biftu T, Sinha-Roy R, Chen P, Qian X, Feng D, Kuethe JT, Scapin G, Gao YD, Yan Y, Krueger D, Bak A, Eiermann G, He J, Cox J, Hicks J, Lyons K, He H, Salituro G, Tong S, Patel S, Doss G, Petrov A, Wu J, Xu SS, Sewall C, Zhang X, Zhang B, Thornberry NA, Weber AE. Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes. J Med Chem. 2014 Apr 24;57(8):3205-12. doi: 10.1021/jm401992e. Epub 2014 Apr 2. PubMed PMID: 24660890.

2: Biftu T, Qian X, Chen P, Feng D, Scapin G, Gao YD, Cox J, Roy RS, Eiermann G,  He H, Lyons K, Salituro G, Patel S, Petrov A, Xu F, Xu SS, Zhang B, Caldwell C, Wu JK, Lyons K, Weber AE. Novel tetrahydropyran analogs as dipeptidyl peptidase IV inhibitors: Profile of clinical candidate (2R,3S,5R)-2- (2,5-difluorophenyl)-5-(4,6-dihydropyrrolo [3,4-c]pyrazol-5-(1H)-yl)tetrahydro-2H-pyran-3-amine (23) [corrected]. Bioorg Med Chem Lett. 2013 Oct 1;23(19):5361-6. doi: 10.1016/j.bmcl.2013.07.061. Epub 2013 Aug 5. Erratum in: Bioorg Med Chem Lett. 2014 Jun 1;24(11):2590. PubMed PMID: 23972441.