Original:Verubecestat TFA 2095432-65-6 , stock more than 100g

EOS med chem is the only manufacturer that provides excellent quality chemistry products and services at affordable rates. The experts working here are highly trained to handle these chemicals used in the creation of medicines used for treating various life-threatening diseases. We are into the manufacturing of chemical products after doing a deep research for the same.

EOS team of experts holds the work experience of more than ten years, and therefore we can assure you about the quality and superiority of the products and services we offer to all our valued clients around the globe. At present, this organization is listed among the most leading pharmaceutical suppliers around the world. We always supply products keeping the affordability in mind.

2018 CHINA CPHI, W4E82

Description: Verubecestat, also known as MK-8931 or SCH 900931, is a potent and selective beta-secretase inhibitor, and BACE1 protein inhibitor or Beta-site APP-cleaving enzyme 1 inhibitor. Verubecestat is a promising novel therapeutic drug candidate in Alzheimer's disease. Verubecestat reduced Aβ cerebral spinal fluids (CSF) levels up to 92% and was well tolerated by patients.

Name: Verubecestat TFA 

CAS#: 2095432-65-6 (TFA) 

Chemical Formula: C19H18F5N5O5S 

Exact Mass: 409.102 

Molecular Weight: 523.435 

Elemental Analysis: C, 43.60; H, 3.47; F, 18.15; N, 13.38; O, 15.28; S, 6.12

Related CAS #: 2095432-65-6 (TFA)   1286770-55-5 (free base)   1875153-95-9 (Tosylate)   1970144-54-7 (HBr)   1897370-45-4 (hydrate)  

Synonym: MK-8931; MK 8931; MK8931; MK-8931-009; SCH 900931; SCH-900931; SCH900931; Verubecestat TFA;

IUPAC/Chemical Name: (R)-N-(3-(3-amino-2,5-dimethyl-1,1-dioxido-5,6-dihydro-2H-1,2,4-thiadiazin-5-yl)-4-fluorophenyl)-5-fluoropicolinamide trifluoroacetic acid

InChi Key: MNYVOIVLGITLBF-LMOVPXPDSA-N

InChi Code: InChI=1S/C17H17F2N5O3S.C2HF3O2/c1-17(9-28(26,27)24(2)16(20)23-17)12-7-11(4-5-13(12)19)22-15(25)14-6-3-10(18)8-21-14;3-2(4,5)1(6)7/h3-8H,9H2,1-2H3,(H2,20,23)(H,22,25);(H,6,7)/t17-;/m0./s1

SMILES Code: O=C(NC1=CC=C(F)C([C@@](C2)(C)N=C(N)N(C)S2(=O)=O)=C1)C3=NC=C(F)C=C3.O=C(O)C(F)(F)F

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code: 293490

REFERENCES

1: Thaisrivongs DA, Morris WJ, Tan L, Song ZJ, Lyons TW, Waldman JH, Naber JR, Chen W, Chen L, Zhang B, Yang J. A Next Generation Synthesis of BACE1 Inhibitor Verubecestat (MK-8931). Org Lett. 2018 Mar 16;20(6):1568-1571. doi: 10.1021/acs.orglett.8b00259. Epub 2018 Feb 26. PubMed PMID: 29481097.

2: Chen W, Meng D, N'Zemba B, Morris WJ. Palladium-Catalyzed Enantioselective Synthesis of Cyclic Sulfamidates and Application to a Synthesis of Verubecestat. Org Lett. 2018 Mar 2;20(5):1265-1268. doi: 10.1021/acs.orglett.7b03639. Epub 2018 Feb 20. PubMed PMID: 29461065.

3: Barhate CL, Lopez DA, Makarov AA, Bu X, Morris WJ, Lekhal A, Hartman R, Armstrong DW, Regalado EL. Macrocyclic glycopeptide chiral selectors bonded to core-shell particles enables enantiopurity analysis of the entire verubecestat synthetic route. J Chromatogr A. 2018 Mar 2;1539:87-92. doi: 10.1016/j.chroma.2018.01.042. Epub 2018 Jan 31. PubMed PMID: 29397980.

4: Geerts H, Spiros A, Roberts P. Impact of amyloid-beta changes on cognitive outcomes in Alzheimer's disease: analysis of clinical trials using a quantitative systems pharmacology model. Alzheimers Res Ther. 2018 Feb 2;10(1):14. doi: 10.1186/s13195-018-0343-5. PubMed PMID: 29394903; PubMed Central PMCID: PMC5797372.

5: Villarreal S, Zhao F, Hyde LA, Holder D, Forest T, Sondey M, Chen X, Sur C, Parker EM, Kennedy ME. Chronic Verubecestat Treatment Suppresses Amyloid Accumulation in Advanced Aged Tg2576-AβPPswe Mice Without Inducing Microhemorrhage. J Alzheimers Dis. 2017;59(4):1393-1413. doi: 10.3233/JAD-170056. PubMed PMID: 28800329; PubMed Central PMCID: PMC5611839.

6: Prati F, Bottegoni G, Bolognesi ML, Cavalli A. BACE-1 Inhibitors: From Recent Single-Target Molecules to Multitarget Compounds for Alzheimer's Disease. J Med Chem. 2018 Feb 8;61(3):619-637. doi: 10.1021/acs.jmedchem.7b00393. Epub 2017 Aug 8. PubMed PMID: 28749667.

7: Hung SY, Fu WM. Drug candidates in clinical trials for Alzheimer's disease. J Biomed Sci. 2017 Jul 19;24(1):47. doi: 10.1186/s12929-017-0355-7. Review. PubMed PMID: 28720101; PubMed Central PMCID: PMC5516350.

8: Mullard A. BACE inhibitor bust in Alzheimer trial. Nat Rev Drug Discov. 2017 Mar 1;16(3):155. doi: 10.1038/nrd.2017.43. PubMed PMID: 28248932.

9: Hawkes N. Merck ends trial of potential Alzheimer's drug verubecestat. BMJ. 2017 Feb 15;356:j845. doi: 10.1136/bmj.j845. PubMed PMID: 28202490.

10: Thaisrivongs DA, Miller SP, Molinaro C, Chen Q, Song ZJ, Tan L, Chen L, Chen W, Lekhal A, Pulicare SK, Xu Y. Synthesis of Verubecestat, a BACE1 Inhibitor for the Treatment of Alzheimer's Disease. Org Lett. 2016 Nov 18;18(22):5780-5783. Epub 2016 Nov 4. PubMed PMID: 27934506.

11: Scott JD, Li SW, Brunskill AP, Chen X, Cox K, Cumming JN, Forman M, Gilbert EJ, Hodgson RA, Hyde LA, Jiang Q, Iserloh U, Kazakevich I, Kuvelkar R, Mei H, Meredith J, Misiaszek J, Orth P, Rossiter LM, Slater M, Stone J, Strickland CO, Voigt JH, Wang G, Wang H, Wu Y, Greenlee WJ, Parker EM, Kennedy ME, Stamford AW. Discovery of the 3-Imino-1,2,4-thiadiazinane 1,1-Dioxide Derivative Verubecestat (MK-8931)-A β-Site Amyloid Precursor Protein Cleaving Enzyme 1 Inhibitor for the Treatment of Alzheimer's Disease. J Med Chem. 2016 Dec 8;59(23):10435-10450. Epub 2016 Nov 18. PubMed PMID: 27933948.

12: Kennedy ME, Stamford AW, Chen X, Cox K, Cumming JN, Dockendorf MF, Egan M, Ereshefsky L, Hodgson RA, Hyde LA, Jhee S, Kleijn HJ, Kuvelkar R, Li W, Mattson BA, Mei H, Palcza J, Scott JD, Tanen M, Troyer MD, Tseng JL, Stone JA, Parker EM, Forman MS. The BACE1 inhibitor verubecestat (MK-8931) reduces CNS β-amyloid in animal models and in Alzheimer's disease patients. Sci Transl Med. 2016 Nov 2;8(363):363ra150. PubMed PMID: 27807285.

13: Panza F, Seripa D, Solfrizzi V, Imbimbo BP, Lozupone M, Leo A, Sardone R, Gagliardi G, Lofano L, Creanza BC, Bisceglia P, Daniele A, Bellomo A, Greco A, Logroscino G. Emerging drugs to reduce abnormal β-amyloid protein in Alzheimer's disease patients. Expert Opin Emerg Drugs. 2016 Dec;21(4):377-391. Epub 2016 Oct 6. Review. PubMed PMID: 27678025.

14: Yan R. Stepping closer to treating Alzheimer's disease patients with BACE1 inhibitor drugs. Transl Neurodegener. 2016 Jul 14;5:13. doi: 10.1186/s40035-016-0061-5. eCollection 2016. Review. PubMed PMID: 27418961; PubMed Central PMCID: PMC4944430.

15: Evin G. Future Therapeutics in Alzheimer's Disease: Development Status of BACE Inhibitors. BioDrugs. 2016 Jun;30(3):173-94. doi: 10.1007/s40259-016-0168-3. Review. PubMed PMID: 27023706.

Original:YM-90709 163769-88-8 , stock more than 100g

EOS med chem is the only manufacturer that provides excellent quality chemistry products and services at affordable rates. The experts working here are highly trained to handle these chemicals used in the creation of medicines used for treating various life-threatening diseases. We are into the manufacturing of chemical products after doing a deep research for the same.

EOS team of experts holds the work experience of more than ten years, and therefore we can assure you about the quality and superiority of the products and services we offer to all our valued clients around the globe. At present, this organization is listed among the most leading pharmaceutical suppliers around the world. We always supply products keeping the affordability in mind.

2018 CHINA CPHI, W4E82

EOS Med Chem, Medchem is Big
執大象，天下往，往而無害，安平泰
WEB: www.eosmedchem.com
EMAIL: info@eosmedchem.com; eosmedchem@gmail.com; eosmedchem@qq.com  
TEL: 0086-531-69905422
GMP PLANT: No. 37, Yulong Road, Qufu City, Shandong Province.

Description: YM-90709 is an interleukin-5 receptor antagonist. YM-90709 inhibits the binding of IL-5 to its receptor on peripheral human eosinophils and butyric acid-treated eosinophilic HL-60 clone 15 cells, with IC50 values of 1.0 and 0.57 microM, respectively. In functional assays, YM-90709 inhibited IL-5-prolonged eosinophil survival with an IC50 value of 0.45 microM and did not affect the GM-CSF-prolonged eosinophil survival. Furthermore, YM-90709 inhibited the IL-5-induced but not GM-CSF-induced tyrosine phosphorylation of Janus kinase 2 (JAK2) in eosinophilic HL-60 clone 15 cells.

Name: YM-90709 

CAS#: 163769-88-8 

Chemical Formula: C22H21N3O2 

Exact Mass: 359.1634 

Molecular Weight: 359.429 

Elemental Analysis: C, 73.52; H, 5.89; N, 11.69; O, 8.90

Synonym: YM-90709; YM 90709; YM90709.

IUPAC/Chemical Name: 2,3-dimethoxy-6,6-dimethyl-5,6-dihydrobenzo[7,8]indolizino[2,3-b]quinoxaline

InChi Key: HIXSPVQXXDULHS-UHFFFAOYSA-N

InChi Code: InChI=1S/C22H21N3O2/c1-22(2)12-13-9-19(26-3)20(27-4)10-14(13)18-11-17-21(25(18)22)24-16-8-6-5-7-15(16)23-17/h5-11H,12H2,1-4H3

SMILES Code: CC(CC1=CC(OC)=C(OC)C=C12)(C)N3C2=CC4=NC5=CC=CC=C5N=C43

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code: 293490

REFERENCES

1: Morokata T, Suzuki K, Ida K, Yamada T. Effect of a novel interleukin-5 

receptor antagonist, YM-90709, on antigen-induced eosinophil infiltration into 

the airway of BDF1 mice. Immunol Lett. 2005 Apr 15;98(1):161-5. Epub 2004 Nov 28. 

PubMed PMID: 15790522.

2: Morokata T, Suzuki K, Ida K, Tsuchiyama H, Ishikawa J, Yamada T. Effect of a 

novel interleukin-5 receptor antagonist, YM-90709 

(2,3-dimethoxy-6,6-dimethyl-5,6-dihydrobenzo[7,8]indolizino[2,3-b]quinoxaline), 

on antigen-induced airway inflammation in BN rats. Int Immunopharmacol. 2004 

Jul;4(7):873-83. PubMed PMID: 15182727.

3: Morokata T, Ida K, Yamada T. Characterization of YM-90709 as a novel 

antagonist which inhibits the binding of interleukin-5 to interleukin-5 receptor. 

Int Immunopharmacol. 2002 Nov;2(12):1693-702. PubMed PMID: 12469943.

Original:GDC-0853 1434048-34-6 , stock more than 100g

EOS med chem is the only manufacturer that provides excellent quality chemistry products and services at affordable rates. The experts working here are highly trained to handle these chemicals used in the creation of medicines used for treating various life-threatening diseases. We are into the manufacturing of chemical products after doing a deep research for the same.

EOS team of experts holds the work experience of more than ten years, and therefore we can assure you about the quality and superiority of the products and services we offer to all our valued clients around the globe. At present, this organization is listed among the most leading pharmaceutical suppliers around the world. We always supply products keeping the affordability in mind.

2018 CHINA CPHI, W4E82

EOS Med Chem, Medchem is Big
執大象，天下往，往而無害，安平泰
WEB: www.eosmedchem.com
EMAIL: info@eosmedchem.com; eosmedchem@gmail.com; eosmedchem@qq.com  
TEL: 0086-531-69905422
GMP PLANT: No. 37, Yulong Road, Qufu City, Shandong Province.

Description: GDC-0853 is orally available inhibitor of Bruton's tyrosine kinase (BTK) with potential antineoplastic activity. Upon administration, GDC-0853 inhibits the activity of BTK and prevents the activation of the B-cell antigen receptor (BCR) signaling pathway. This prevents both B-cell activation and BTK-mediated activation of downstream survival pathways, which leads to the inhibition of the growth of malignant B-cells that overexpress BTK. BTK, a member of the Src-related BTK/Tec family of cytoplasmic tyrosine kinases, is overexpressed in B-cell malignancies; it plays an important role in B-lymphocyte development, activation, signaling, proliferation and survival.

Name: GDC-0853 

CAS#: 1434048-34-6 

Chemical Formula: C37H44N8O4 

Exact Mass: 664.3486 

Molecular Weight: 664.811 

Elemental Analysis: C, 66.85; H, 6.67; N, 16.86; O, 9.63

Synonym: GDC-0853; GDC 0853; GDC0853; RG-7845; RG7845; RG 7845.

IUPAC/Chemical Name: (S)-2-(3'-(hydroxymethyl)-1-methyl-5-((5-(2-methyl-4-(oxetan-3-yl)piperazin-1-yl)pyridin-2-yl)amino)-6-oxo-1,6-dihydro-[3,4'-bipyridin]-2'-yl)-7,7-dimethyl-3,4,7,8-tetrahydro-2H-cyclopenta[4,5]pyrrolo[1,2-a]pyrazin-1(6H)-one

InChi Key: WNEODWDFDXWOLU-QHCPKHFHSA-N

InChi Code: InChI=1S/C37H44N8O4/c1-23-18-42(27-21-49-22-27)9-10-43(23)26-5-6-33(39-17-26)40-30-13-25(19-41(4)35(30)47)28-7-8-38-34(29(28)20-46)45-12-11-44-31(36(45)48)14-24-15-37(2,3)16-32(24)44/h5-8,13-14,17,19,23,27,46H,9-12,15-16,18,20-22H2,1-4H3,(H,39,40)/t23-/m0/s1

SMILES Code: O=C1C(N2CCN1C3=NC=CC(C(C=C4NC5=NC=C(N6[C@@H](C)CN(C7COC7)CC6)C=C5)=CN(C)C4=O)=C3CO)=CC8=C2CC(C)(C)C8

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code: 293490

ADDITIONAL INFORMATION

Note: Structure was from https://newdrugapprovals.org/2016/03/ ( visited on 4/7/2016)

REFERENCES

Heteroarylpyridone and azapyridone compounds as inhibitors of BTK activity and their preparation 

By Crawford, James John; Ortwine, Daniel Fred; Wei, Binqing; Young, Wendy B. 

From PCT Int. Appl. (2013), WO 2013067274 A1 20130510.

Original: Niraparib free base 1038915-60-4, stock more than 100g

EOS med chem is the only manufacturer that provides excellent quality chemistry products and services at affordable rates. The experts working here are highly trained to handle these chemicals used in the creation of medicines used for treating various life-threatening diseases. We are into the manufacturing of chemical products after doing a deep research for the same.

EOS team of experts holds the work experience of more than ten years, and therefore we can assure you about the quality and superiority of the products and services we offer to all our valued clients around the globe. At present, this organization is listed among the most leading pharmaceutical suppliers around the world. We always supply products keeping the affordability in mind.

2018 CHINA CPHI, W4E82

EOS Med Chem, Medchem is Big
執大象，天下往，往而無害，安平泰
WEB: www.eosmedchem.com
EMAIL: info@eosmedchem.com; eosmedchem@gmail.com; eosmedchem@qq.com  
TEL: 0086-531-69905422
GMP PLANT: No. 37, Yulong Road, Qufu City, Shandong Province.

Description: Niraparib, also known as MK4827, is an orally active, potent and selective poly(ADP-Ribose) polymerase (PARP) inhibitor that radiosensitizes human lung and breast cancer cells. Niraparib inhibits PARP1/PARP2 with IC50 of 3.8 nM/2.1 nM respectively. Niraparib is currently in Phase 3 clinical trials for ovarian cancer and BRCA+ breast cancer.

Name: Niraparib free base 

CAS#: 1038915-60-4 (free base) 

Chemical Formula: C19H20N4O 

Exact Mass: 320.1637 

Molecular Weight: 320.396 

Elemental Analysis: C, 71.23; H, 6.29; N, 17.49; O, 4.99

Related CAS #: 1038915-60-4 (free base)   1038915-64-8 (HCl)   1038915-73-9 (tosylate)   1613220-15-7 (tosylate hydrate)  

Synonym: MK-4827; MK 4827; MK4827; Niraparib. Niraparib free base.

IUPAC/Chemical Name: (S)-2-(4-(piperidin-3-yl)phenyl)-2H-indazole-7-carboxamide

InChi Key: PCHKPVIQAHNQLW-CQSZACIVSA-N

InChi Code: InChI=1S/C19H20N4O/c20-19(24)17-5-1-3-15-12-23(22-18(15)17)16-8-6-13(7-9-16)14-4-2-10-21-11-14/h1,3,5-9,12,14,21H,2,4,10-11H2,(H2,20,24)/t14-/m1/s1

SMILES Code: O=C(C1=CC=CC2=CN(C3=CC=C([C@H]4CNCCC4)C=C3)N=C12)N

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code: 293490

ADDITIONAL INFORMATION

REFERENCES

1: Ledermann JA. PARP inhibitors in ovarian cancer. Ann Oncol. 2016 Apr;27 Suppl 1:i40-i44. doi: 10.1093/annonc/mdw094. PubMed PMID: 27141070.

2: Kaye SB. Progress in the treatment of ovarian cancer-lessons from homologous recombination deficiency-the first 10 years. Ann Oncol. 2016 Apr;27 Suppl 1:i1-i3. doi: 10.1093/annonc/mdw082. PubMed PMID: 27141062; PubMed Central PMCID: PMC4852273.

3: Jenner ZB, Sood AK, Coleman RL. Evaluation of rucaparib and companion diagnostics in the PARP inhibitor landscape for recurrent ovarian cancer therapy. Future Oncol. 2016 Jun;12(12):1439-56. doi: 10.2217/fon-2016-0002. Epub 2016 Apr 18. PubMed PMID: 27087632.

4: Liu JF, Matulonis UA. What Is the Place of PARP Inhibitors in Ovarian Cancer Treatment? Curr Oncol Rep. 2016 May;18(5):29. doi: 10.1007/s11912-016-0515-z. Review. PubMed PMID: 26984416.

5: Alotaibi M, Sharma K, Saleh T, Povirk LF, Hendrickson EA, Gewirtz DA. Radiosensitization by PARP Inhibition in DNA Repair Proficient and Deficient Tumor Cells: Proliferative Recovery in Senescent Cells. Radiat Res. 2016 Mar;185(3):229-45. doi: 10.1667/RR14202.1. Epub 2016 Mar 2. PubMed PMID: 26934368; PubMed Central PMCID: PMC4821451.

6: Ekblad T, Schüler H. Sirtuins are Unaffected by PARP Inhibitors Containing Planar Nicotinamide Bioisosteres. Chem Biol Drug Des. 2016 Mar;87(3):478-82. doi: 10.1111/cbdd.12680. Epub 2015 Nov 26. PubMed PMID: 26518726.

7: McGonigle S, Chen Z, Wu J, Chang P, Kolber-Simonds D, Ackermann K, Twine NC, Shie JL, Miu JT, Huang KC, Moniz GA, Nomoto K. E7449: A dual inhibitor of PARP1/2 and tankyrase1/2 inhibits growth of DNA repair deficient tumors and antagonizes Wnt signaling. Oncotarget. 2015 Dec 1;6(38):41307-23. doi: 10.18632/oncotarget.5846. PubMed PMID: 26513298; PubMed Central PMCID: PMC4747407.

8: Engert F, Schneider C, Weiβ LM, Probst M, Fulda S. PARP Inhibitors Sensitize Ewing Sarcoma Cells to Temozolomide-Induced Apoptosis via the Mitochondrial Pathway. Mol Cancer Ther. 2015 Dec;14(12):2818-30. doi: 10.1158/1535-7163.MCT-15-0587. Epub 2015 Oct 5. PubMed PMID: 26438158.

9: Chornenkyy Y, Agnihotri S, Yu M, Buczkowicz P, Rakopoulos P, Golbourn B, Garzia L, Siddaway R, Leung S, Rutka JT, Taylor MD, Dirks PB, Hawkins C. Poly-ADP-Ribose Polymerase as a Therapeutic Target in Pediatric Diffuse Intrinsic Pontine Glioma and Pediatric High-Grade Astrocytoma. Mol Cancer Ther. 2015 Nov;14(11):2560-8. doi: 10.1158/1535-7163.MCT-15-0282. Epub 2015 Sep 8. PubMed PMID: 26351319.

10: Seimiya H. [Cancer therapy by PARP inhibitors]. Nihon Rinsho. 2015 Aug;73(8):1330-5. Review. Japanese. PubMed PMID: 26281686.

11: Hopkins TA, Shi Y, Rodriguez LE, Solomon LR, Donawho CK, DiGiammarino EL, Panchal SC, Wilsbacher JL, Gao W, Olson AM, Stolarik DF, Osterling DJ, Johnson EF, Maag D. Mechanistic Dissection of PARP1 Trapping and the Impact on In Vivo Tolerability and Efficacy of PARP Inhibitors. Mol Cancer Res. 2015 Nov;13(11):1465-77. doi: 10.1158/1541-7786.MCR-15-0191-T. Epub 2015 Jul 27. PubMed PMID: 26217019.

12: Jones P, Wilcoxen K, Rowley M, Toniatti C. Niraparib: A Poly(ADP-ribose) Polymerase (PARP) Inhibitor for the Treatment of Tumors with Defective Homologous Recombination. J Med Chem. 2015 Apr 23;58(8):3302-14. doi: 10.1021/jm5018237. Epub 2015 Mar 11. PubMed PMID: 25761096.

13: Shen Y, Aoyagi-Scharber M, Wang B. Trapping Poly(ADP-Ribose) Polymerase. J Pharmacol Exp Ther. 2015 Jun;353(3):446-57. doi: 10.1124/jpet.114.222448. Epub 2015 Mar 10. PubMed PMID: 25758918.

14: Genther Williams SM, Kuznicki AM, Andrade P, Dolinski BM, Elbi C, O'Hagan RC, Toniatti C. Treatment with the PARP inhibitor, niraparib, sensitizes colorectal cancer cell lines to irinotecan regardless of MSI/MSS status. Cancer Cell Int. 2015 Feb 4;15(1):14. doi: 10.1186/s12935-015-0162-8. eCollection 2015. PubMed PMID: 25685067; PubMed Central PMCID: PMC4326439.

15: Bridges KA, Toniatti C, Buser CA, Liu H, Buchholz TA, Meyn RE. Niraparib (MK-4827), a novel poly(ADP-Ribose) polymerase inhibitor, radiosensitizes human lung and breast cancer cells. Oncotarget. 2014 Jul 15;5(13):5076-86. PubMed PMID: 24970803; PubMed Central PMCID: PMC4148123.

16: Liu JF, Konstantinopoulos PA, Matulonis UA. PARP inhibitors in ovarian cancer: current status and future promise. Gynecol Oncol. 2014 May;133(2):362-9. doi: 10.1016/j.ygyno.2014.02.039. Epub 2014 Mar 4. Review. PubMed PMID: 24607283.

17: Murai J, Huang SY, Renaud A, Zhang Y, Ji J, Takeda S, Morris J, Teicher B, Doroshow JH, Pommier Y. Stereospecific PARP trapping by BMN 673 and comparison with olaparib and rucaparib. Mol Cancer Ther. 2014 Feb;13(2):433-43. doi: 10.1158/1535-7163.MCT-13-0803. Epub 2013 Dec 19. PubMed PMID: 24356813; PubMed Central PMCID: PMC3946062.

18: Reinbolt RE, Hays JL. The Role of PARP Inhibitors in the Treatment of Gynecologic Malignancies. Front Oncol. 2013 Oct 1;3:237. doi: 10.3389/fonc.2013.00237. Review. PubMed PMID: 24098868; PubMed Central PMCID: PMC3787651.

19: Postel-Vinay S, Bajrami I, Friboulet L, Elliott R, Fontebasso Y, Dorvault N, Olaussen KA, André F, Soria JC, Lord CJ, Ashworth A. A high-throughput screen identifies PARP1/2 inhibitors as a potential therapy for ERCC1-deficient non-small cell lung cancer. Oncogene. 2013 Nov 21;32(47):5377-87. doi: 10.1038/onc.2013.311. Epub 2013 Aug 12. PubMed PMID: 23934192.

20: Infante JR, Burris HA 3rd. PARP inhibitors: pitfalls and promises. Lancet Oncol. 2013 Aug;14(9):798-9. doi: 10.1016/S1470-2045(13)70276-6. Epub 2013 Jun 28. PubMed PMID: 23810789.

Original: Avadomide free base 1015474-32-4 , stock more than 100g

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Description: Avadomide, also known as CC-122, is an orally available pleiotropic pathway modulator with potential antineoplastic activity. CC-122 mimics an interferon response and has antitumor activity in DLBCL CC-122 binds Cereblon (CRBN) and promotes degradation of Aiolos and Ikaros in diffuse large B-cell lymphoma (DLBCL) and T cells in vitro, in vivo, and in patients, resulting in both cell autonomous as well as immunostimulatory effects.

Name: Avadomide free base 

CAS#: 1015474-32-4 (free base) 

Chemical Formula: C14H14N4O3 

Exact Mass: 286.1066 

Molecular Weight: 286.291 

Elemental Analysis: C, 58.74; H, 4.93; N, 19.57; O, 16.77

Related CAS #: 1398053-45-6 (HCl)   1015474-32-4 (free base)    

Synonym: CC 122; CC-122; CC122, Avadomide

IUPAC/Chemical Name: 3-(5-amino-2-methyl-4-oxoquinazolin-3(4H)-yl)piperidine-2,6-dione

InChi Key: RSNPAKAFCAAMBH-UHFFFAOYSA-N

InChi Code: InChI=1S/C14H14N4O3/c1-7-16-9-4-2-3-8(15)12(9)14(21)18(7)10-5-6-11(19)17-13(10)20/h2-4,10H,5-6,15H2,1H3,(H,17,19,20)

SMILES Code: O=C(C(N1C(C)=NC2=C(C(N)=CC=C2)C1=O)CC3)NC3=O

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >5 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code: 293490

ADDITIONAL INFORMATION

 In DLBCL cell lines, CC-122-induced degradation or short hairpin RNA-mediated knockdown of Aiolos and Ikaros correlates with increased transcription of interferon (IFN)-stimulated genes independent of IFN-α, -β, and -γ production and/or secretion and results in apoptosis in both activated B-cell (ABC) and germinal center B-cell DLBCL 

  

REFERENCES

1: Hagner PR, Man HW, Fontanillo C, Wang M, Couto S, Breider M, Bjorklund C, Havens CG, Lu G, Rychak E, Raymon H, Narla RK, Barnes L, Khambatta G, Chiu H, Kosek J, Kang J, Amantangelo MD, Waldman M, Lopez-Girona A, Cai T, Pourdehnad M, Trotter M, Daniel TO, Schafer PH, Klippel A, Thakurta A, Chopra R, Gandhi AK. CC-122, a pleiotropic pathway modifier, mimics an interferon response and has antitumor activity in DLBCL. Blood. 2015 Aug 6;126(6):779-89. doi: 10.1182/blood-2015-02-628669. Epub 2015 May 22. PubMed PMID: 26002965; PubMed Central PMCID: PMC4528065.

2: Li Y, Carayannopoulos LN, Thomas M, Palmisano M, Zhou S. Exposure-response analysis to assess the concentration-QTc relationship of CC-122. Clin Pharmacol. 2016 Sep 9;8:117-25. doi: 10.2147/CPAA.S111867. eCollection 2016. PubMed PMID: 27672344; PubMed Central PMCID: PMC5024774.

3: Krönke J, Fink EC, Hollenbach PW, MacBeth KJ, Hurst SN, Udeshi ND, Chamberlain PP, Mani DR, Man HW, Gandhi AK, Svinkina T, Schneider RK, McConkey M, Järås M, Griffiths E, Wetzler M, Bullinger L, Cathers BE, Carr SA, Chopra R, Ebert BL. Lenalidomide induces ubiquitination and degradation of CK1α in del(5q) MDS. Nature. 2015 Jul 9;523(7559):183-188. doi: 10.1038/nature14610. Epub 2015 Jul 1. PubMed PMID: 26131937; PubMed Central PMCID: PMC4853910.

4: Cubillos-Zapata C, Cordoba R, Avendaño-Ortiz J, Arribas-Jiménez C, Hernández-Jiménez E, Toledano V, Villaescusa T, Moreno V, López-Collazo E. CC-122 immunomodulatory effects in refractory patients with diffuse large B-cell lymphoma. Oncoimmunology. 2016 Sep 16;5(12):e1231290. doi: 10.1080/2162402X.2016.1231290. eCollection 2016. PubMed PMID: 28255524; PubMed Central PMCID: PMC5325046.

5: Jacques V, Czarnik AW, Judge TM, Van der Ploeg LH, DeWitt SH. Differentiation of antiinflammatory and antitumorigenic properties of stabilized enantiomers of thalidomide analogs. Proc Natl Acad Sci U S A. 2015 Mar 24;112(12):E1471-9. doi: 10.1073/pnas.1417832112. Epub 2015 Mar 9. Erratum in: Proc Natl Acad Sci U S A. 2015 May 12;112(19):E2553. PubMed PMID: 25775521; PubMed Central PMCID: PMC4378388.

6: Nowakowski GS. Evolution: IMiDs to PPMs, revolution in DLBCL? Blood. 2015 Aug 6;126(6):698-700. doi: 10.1182/blood-2015-06-649483. PubMed PMID: 26251224.

7: Ito T, Handa H. Recent topics in IMiDs and cereblon. Rinsho Ketsueki. 2017;58(10):2067-2073. doi: 10.11406/rinketsu.58.2067. PubMed PMID: 28978850.

8: Camicia R, Winkler HC, Hassa PO. Novel drug targets for personalized precision medicine in relapsed/refractory diffuse large B-cell lymphoma: a comprehensive review. Mol Cancer. 2015 Dec 11;14:207. doi: 10.1186/s12943-015-0474-2. Review. PubMed PMID: 26654227; PubMed Central PMCID: PMC4676894.

9: Cubillos-Zapata C, Córdoba R, Avendaño-Ortiz J, Lopez-Collazo E. Thalidomide analog CC-122 induces a refractory state in monocytes from patients with diffuse large B cell lymphoma. Leuk Lymphoma. 2017 Aug;58(8):1999-2001. doi: 10.1080/10428194.2016.1272686. Epub 2017 Jan 16. Retraction in: Leuk Lymphoma. 2017 Aug;58(8):I. PubMed PMID: 28093007.