EOS Med Chem, Medicinal Chemical is Big

2018年5月4日星期五

GMP Manufacturer: Ivosidenib; AG-120 (CAS 1448347-49-6) and intermediates.

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.

Welcome, 2018 CHINA CPHI, W4E82

EOS Med Chem, Medchem is Big
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Ivosidenib; AG-120 (CAS 1448347-49-6) : HPLC99.2%, LCMS, NMR, ROS, MOA, COA is ok, stock more than 10G.

Name: Ivosidenib

CAS#: 1448347-49-6 (Ivosidenib)

Chemical Formula: C28H22ClF3N6O3

Exact Mass: 582.1394

Molecular Weight: 582.97

Elemental Analysis: C, 57.69; H, 3.80; Cl, 6.08; F, 9.78; N, 14.42; O, 8.23

Related CAS #: 1448347-49-6 (Ivosidenib) 1448346-63-1 (AG-120 racemic)

Synonym: Ivosidenib, AG-120

IUPAC/Chemical Name: (S)-N-((S)-1-(2-chlorophenyl)-2-((3,3-difluorocyclobutyl)amino)-2-oxoethyl)-1-(4-cyanopyridin-2-yl)-N-(5-fluoropyridin-3-yl)-5-oxopyrrolidine-2-carboxamide

InChi Key: WIJZXSAJMHAVGX-DHLKQENFSA-N

SMILES Code: O=C([C@H](CC1)N(C2=NC=CC(C#N)=C2)C1=O)N([C@@H](C3=CC=CC=C3Cl)C(NC4CC(F)(F)C4)=O)C5=CC(F)=CN=C5

Ivosidenib; AG-120 (CAS 1448347-49-6) Intermeidates:

Ivosidenib intermediate：dipropan-2-yl 3,3-dimethoxycyclobutane-1,1-dicarboxylate,

CAS# 115118-68-8, HPLC 99%, LCMS, HNMR, ROS, MOA, COA is ok, stock more than 1KG.

Ivosidenib intermediate：3-oxocyclobutane-1-carboxylic acid,

CAS# 23761-23-1, HPLC 99%, LCMS, HNMR, ROS, MOA, COA is ok, stock more than 1KG.

Ivosidenib intermediate：3,3-difluorocyclobutanamine hydrochloride,

CAS# 637031-93-7, HPLC 99%, LCMS, HNMR, ROS, MOA, COA is ok, stock more than 1KG.

Ivosidenib intermediate：2-Chlorobenzaldehyde,

CAS# 89-98-5, HPLC 99%, LCMS, HNMR, ROS, MOA, COA is ok, stock more than 1KG.

Ivosidenib intermediate：3-AMINO-5-FLUOROPYRIDINE,

CAS# 210169-05-4, HPLC 99%, LCMS, HNMR, ROS, MOA, COA is ok, stock more than 1KG.

Ivosidenib intermediate：L-Pyroglutamic acid,

CAS# 98-79-3, HPLC 99%, LCMS, HNMR, ROS, MOA, COA is ok, stock more than 10KG.

Ivosidenib intermediate：3,3-DIFLUORO-CYCLOBUTANECARBONITRILE,

CAS# 86770-80-1, HPLC 99%, LCMS, HNMR, ROS, MOA, COA is ok, stock more than 10KG.

Ivosidenib intermediate：2-Bromo-4-cyanopyridine,

CAS# 10386-27-3, HPLC 99%, LCMS, HNMR, ROS, MOA, COA is ok, stock more than 10KG.

REFERENCES

1: Birendra KC, DiNardo CD. Evidence for Clinical Differentiation and Differentiation Syndrome in Patients With Acute Myeloid Leukemia and IDH1 Mutations Treated With the Targeted Mutant IDH1 Inhibitor, AG-120. Clin Lymphoma Myeloma Leuk. 2016 Aug;16(8):460-5. doi: 10.1016/j.clml.2016.04.006. PubMed PMID: 27245312; PubMed Central PMCID: PMC4983480.

2: Brody JR, Yabar CS, Zarei M, Bender J, Matrisian LM, Rahib L, Heartwell C, Mason K, Yeo CJ, Peiper SC, Jiang W, Varieur K, Madhavan S, Petricoin E 3rd, Fortuna D, Curtis M, Wang ZX, Pishvaian MJ, Winter JM. Identification of a novel metabolic-related mutation (IDH1) in metastatic pancreatic cancer. Cancer Biol Ther. 2016 Jul 28:0. [Epub ahead of print] PubMed PMID: 27466707.

3: Caino MC, Altieri DC. Molecular Pathways: Mitochondrial Reprogramming in Tumor Progression and Therapy. Clin Cancer Res. 2016 Feb 1;22(3):540-5. doi: 10.1158/1078-0432.CCR-15-0460. Review. PubMed PMID: 26660517; PubMed Central PMCID: PMC4738153.

4: Chen J, Yang J, Cao P. The Evolving Landscape in the Development of Isocitrate Dehydrogenase Mutant Inhibitors. Mini Rev Med Chem. 2016;16(16):1344-1358. PubMed PMID: 27292784.

5: Cuyàs E, Fernández-Arroyo S, Corominas-Faja B, Rodríguez-Gallego E, Bosch-Barrera J, Martin-Castillo B, De Llorens R, Joven J, Menendez JA. Oncometabolic mutation IDH1 R132H confers a metformin-hypersensitive phenotype. Oncotarget. 2015 May 20;6(14):12279-96. PubMed PMID: 25980580; PubMed Central PMCID: PMC4494938.

6: IDH1 inhibitor shows promising early results. Cancer Discov. 2015 Jan;5(1):4. doi: 10.1158/2159-8290.CD-NB2014-178. PubMed PMID: 25583779.

7: Lippi G, Franchini M, Targher G, Poli G, Guidi GC. The significance of evaluating conventional inflammatory markers in Von Willebrand factor measurement. Clin Chim Acta. 2007 Jun;381(2):167-70. PubMed PMID: 17433810.

8: Mayer A, Schatz GC. Enhanced polarizability of aromatic molecules placed in the vicinity of silver clusters. J Phys Condens Matter. 2009 Aug 12;21(32):325301. doi: 10.1088/0953-8984/21/32/325301. PubMed PMID: 21693964.

9: Mayer A, González AL, Aikens CM, Schatz GC. A charge-dipole interaction model for the frequency-dependent polarizability of silver clusters. Nanotechnology. 2009 May 13;20(19):195204. doi: 10.1088/0957-4484/20/19/195204. PubMed PMID: 19420635.

10: Yang X, Cai W, Shao X. Structural variation of silver clusters from Ag13 to Ag160. J Phys Chem A. 2007 Jun 14;111(23):5048-56. PubMed PMID: 17516636.

Original:MSX-130 4051-59-6 , stock more than 100g

2018 CHINA CPHI, W4E82

Description: MSX-130 is CXCR4 Antagonist.

Name: MSX-130

CAS#: 4051-59-6

Chemical Formula: C36H26N4

Exact Mass: 514.2157

Molecular Weight: 514.632

Elemental Analysis: C, 84.02; H, 5.09; N, 10.89

Synonym: MSX-130; MSX 130; MSX130.

IUPAC/Chemical Name: 2,2'-(1,4-Phenylene)bis[4,5-diphenyl-1H-imidazole]

InChi Key: MKRQQXYFSWSAIS-UHFFFAOYSA-N

InChi Code: InChI=1S/C36H26N4/c1-5-13-25(14-6-1)31-32(26-15-7-2-8-16-26)38-35(37-31)29-21-23-30(24-22-29)36-39-33(27-17-9-3-10-18-27)34(40-36)28-19-11-4-12-20-28/h1-24H,(H,37,38)(H,39,40)

SMILES Code: C1(C2=NC(C3=CC=CC=C3)=C(C4=CC=CC=C4)N2)=CC=C(C5=NC(C6=CC=CC=C6)=C(C7=CC=CC=C7)N5)C=C1

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

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

Original:E6446 HCl 1345675-25-3, stock more than 100g

2018 CHINA CPHI, W4E82

Description: E6446 is a synthetic antagonist of nucleic acid-sensing TLRs. , In vitro, low doses of E6446 specifically inhibited the activation of human and mouse TLR9. Tenfold higher concentrations of this compound also inhibited the human TLR8 response to single-stranded RNA. In vivo, therapy with E6446 diminished the activation of TLR9 and prevented the exacerbated cytokine response observed during acute Plasmodium infection. Furthermore, severe signs of ECM, such as limb paralysis, brain vascular leak, and death, were all prevented by oral treatment with E6446.

Name: E6446 HCl

CAS#: 1345675-25-3 (HCl)

Chemical Formula: C27H37Cl2N3O3

Exact Mass:

Molecular Weight: 522.511

Elemental Analysis: C, 62.07; H, 7.14; Cl, 13.57; N, 8.04; O, 9.19

Related CAS #: 1219925-73-1 (free base) 1345675-25-3 (HCl)

Synonym: E6446 HCl; E6446; E-6446; E6446 hydrochloride

IUPAC/Chemical Name: 6-(3-pyrrolidin-1-ylpropoxy)-2-[4-(3-pyrrolidin-1-ylpropoxy)phenyl]-1,3-benzoxazole;dihydrochloride

InChi Key: DQOUZINBHKWGGM-UHFFFAOYSA-N

InChi Code: InChI=1S/C27H35N3O3.2ClH/c1-2-14-29(13-1)17-5-19-31-23-9-7-22(8-10-23)27-28-25-12-11-24(21-26(25)33-27)32-20-6-18-30-15-3-4-16-30;;/h7-12,21H,1-6,13-20H2;2*1H

SMILES Code: [H]Cl.[H]Cl.C1(C2=CC=C(OCCCN3CCCC3)C=C2)=NC4=CC=C(OCCCN5CCCC5)C=C4O1

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

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: Franklin BS, Ishizaka ST, Lamphier M, Gusovsky F, Hansen H, Rose J, Zheng W,

Ataíde MA, de Oliveira RB, Golenbock DT, Gazzinelli RT. Therapeutical targeting

of nucleic acid-sensing Toll-like receptors prevents experimental cerebral

malaria. Proc Natl Acad Sci U S A. 2011 Mar 1;108(9):3689-94. doi:

10.1073/pnas.1015406108. Epub 2011 Feb 8. PubMed PMID: 21303985; PubMed Central

PMCID: PMC3048158.

Original:R-IMPP 2133832-83-2, stock more than 100g

2018 CHINA CPHI, W4E82

Description: R-IMPP is an inhibitor of PCSK9 translation. R-IMPP stimulates uptake of LDL-C in hepatoma cells by increasing LDL-R levels, without altering levels of secreted transferrin.

Name: R-IMPP

CAS#: 2133832-83-2 (free base)

Chemical Formula: C24H27N3O2

Exact Mass: 389.2103

Molecular Weight: 389.5

Elemental Analysis: C, 74.01; H, 6.99; N, 10.79; O, 8.22

Related CAS #: 2133832-83-2 (free base) 2173005-10-0 (HCl)

Synonym: R-IMPP; RIMPP; R IMPP

IUPAC/Chemical Name: (R)-N-(isoquinolin-1-yl)-3-(4-methoxyphenyl)-N-(piperidin-3-yl)propanamide

InChi Key: OKTGXQMSOIQCTJ-HXUWFJFHSA-N

InChi Code: InChI=1S/C24H27N3O2/c1-29-21-11-8-18(9-12-21)10-13-23(28)27(20-6-4-15-25-17-20)24-22-7-3-2-5-19(22)14-16-26-24/h2-3,5,7-9,11-12,14,16,20,25H,4,6,10,13,15,17H2,1H3/t20-/m1/s1

SMILES Code: O=C(N(C1=NC=CC2=C1C=CC=C2)[C@H]3CNCCC3)CCC4=CC=C(OC)C=C4

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

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: Petersen DN, Hawkins J, Ruangsiriluk W, Stevens KA, Maguire BA, O'Connell TN, Rocke BN, Boehm M, Ruggeri RB, Rolph T, Hepworth D, Loria PM, Carpino PA. A Small-Molecule Anti-secretagogue of PCSK9 Targets the 80S Ribosome to Inhibit PCSK9 Protein Translation. Cell Chem Biol. 2016 Nov 17;23(11):1362-1371. doi: 10.1016/j.chembiol.2016.08.016. Epub 2016 Oct 13. PubMed PMID: 27746128.

Original: S38093 free base 862896-30-8 , stock more than 100g

2018 CHINA CPHI, W4E82

Description: S38093 is an inverse agonist at histamine H3 receptors. S 38093 displays a moderate affinity for rat, mouse and human H3 receptors (Ki=8.8, 1.44 and 1.2µM, respectively) with no affinity for other histaminergic receptors. In cellular models, the compound was able to antagonize mice H3 receptors (KB=0.65µM) and to suppress cAMP decrease induced by an H3 agonist via human H3 receptors (KB=0.11µM).

Name: S38093 free base

CAS#: 862896-30-8 (free base)

Chemical Formula: C17H24N2O2

Exact Mass: 288.1838

Molecular Weight: 288.391

Elemental Analysis: C, 70.80; H, 8.39; N, 9.71; O, 11.10

Related CAS #: 862896-30-8 (free base) 1222097-72-4 (HCl)

Synonym: S38093 free base; S-38093; S 38093;

IUPAC/Chemical Name: 4-(3-(hexahydrocyclopenta[c]pyrrol-2(1H)-yl)propoxy)benzamide

InChi Key: MRNMYWNBLVJWKG-UHFFFAOYSA-N

InChi Code: InChI=1S/C17H24N2O2/c18-17(20)13-5-7-16(8-6-13)21-10-2-9-19-11-14-3-1-4-15(14)12-19/h5-8,14-15H,1-4,9-12H2,(H2,18,20)

SMILES Code: C1=C(OCCCN2CC3CCCC3C2)C=CC(C(=O)N)=C1

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

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: Chaumette T, Chapuy E, Berrocoso E, Llorca-Torralba M, Bravo L, Mico JA, Chalus M, Eschalier A, Ardid D, Marchand F, Sors A. Effects of S 38093, an antagonist/inverse agonist of histamine H3 receptors, in models of neuropathic pain in rats. Eur J Pain. 2018 Jan;22(1):127-141. doi: 10.1002/ejp.1097. Epub 2017 Sep 6. PubMed PMID: 28877402.

2: Sors A, Panayi F, Bert L, Favale D, Nosjean O, Audinot V, Arrang JM, Buisson B, Steidl E, Delbos JM, Huhtala T, Kontkanen O, Chollet AM, Casara P, Lestage P. Mechanistic characterization of S 38093, a novel inverse agonist at histamine H3 receptors. Eur J Pharmacol. 2017 May 15;803:11-23. doi: 10.1016/j.ejphar.2017.03.013. Epub 2017 Mar 21. PubMed PMID: 28336400.

3: Panayi F, Sors A, Bert L, Martin B, Rollin-Jego G, Billiras R, Carrié I, Albinet K, Danober L, Rogez N, Thomas JY, Pira L, Bertaina-Anglade V, Lestage P. In vivo pharmacological profile of S 38093, a novel histamine H3 receptor inverse agonist. Eur J Pharmacol. 2017 May 15;803:1-10. doi: 10.1016/j.ejphar.2017.03.008. Epub 2017 Mar 14. PubMed PMID: 28315340.

4: Guilloux JP, Samuels BA, Mendez-David I, Hu A, Levinstein M, Faye C, Mekiri M, Mocaer E, Gardier AM, Hen R, Sors A, David DJ. S 38093, a histamine H(3) antagonist/inverse agonist, promotes hippocampal neurogenesis and improves context discrimination task in aged mice. Sci Rep. 2017 Feb 20;7:42946. doi: 10.1038/srep42946. PubMed PMID: 28218311; PubMed Central PMCID: PMC5317168.

5: Sors A, Krazem A, Kehr J, Yoshitake T, Dominguez G, Henkous N, Letondor C, Mocaer E, Béracochéa DJ. The Synergistic Enhancing-Memory Effect of Donepezil and S 38093 (a Histamine H(3) Antagonist) Is Mediated by Increased Neural Activity in the Septo-hippocampal Circuitry in Middle-Aged Mice. Front Pharmacol. 2016 Dec 22;7:492. doi: 10.3389/fphar.2016.00492. eCollection 2016. PubMed PMID: 28066242; PubMed Central PMCID: PMC5177663.

Original:HSF1A 1196723-93-9 , stock more than 100g

2018 CHINA CPHI, W4E82

Description: HSF1A is an activator of Heat shock transcription factor 1 (HSF1).

Name: HSF1A

CAS#: 1196723-93-9

Chemical Formula: C21H19N3O2S2

Exact Mass: 409.0919

Molecular Weight: 409.522

Elemental Analysis: C, 61.59; H, 4.68; N, 10.26; O, 7.81; S, 15.66

Synonym: HSF1A;

IUPAC/Chemical Name: 4-Ethyl-N-[1-phenyl-3-(2-thienyl)-1H-pyrazol-5-yl]-benzenesulfonamide

InChi Key: KJTITGSAONQVPY-UHFFFAOYSA-N

InChi Code: InChI=1S/C21H19N3O2S2/c1-2-16-10-12-18(13-11-16)28(25,26)23-21-15-19(20-9-6-14-27-20)22-24(21)17-7-4-3-5-8-17/h3-15,23H,2H2,1H3

SMILES Code: O=S(C1=CC=C(CC)C=C1)(NC2=CC(C3=CC=CS3)=NN2C4=CC=CC=C4)=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

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: Huang CY, Kuo WW, Lo JF, Ho TJ, Pai PY, Chiang SF, Chen PY, Tsai FJ, Tsai CH, Huang CY. Doxorubicin attenuates CHIP-guarded HSF1 nuclear translocation and protein stability to trigger IGF-IIR-dependent cardiomyocyte death. Cell Death Dis. 2016 Nov 3;7(11):e2455. doi: 10.1038/cddis.2016.356. PubMed PMID: 27809308; PubMed Central PMCID: PMC5260882.

2: Bocchini CE, Nahmod K, Katsonis P, Kim S, Kasembeli MM, Freeman A, Lichtarge O, Makedonas G, Tweardy DJ. Protein stabilization improves STAT3 function in autosomal dominant hyper-IgE syndrome. Blood. 2016 Dec 29;128(26):3061-3072. doi: 10.1182/blood-2016-02-702373. Epub 2016 Oct 31. PubMed PMID: 27799162; PubMed Central PMCID: PMC5201093.

3: Neef DW, Jaeger AM, Gomez-Pastor R, Willmund F, Frydman J, Thiele DJ. A direct regulatory interaction between chaperonin TRiC and stress-responsive transcription factor HSF1. Cell Rep. 2014 Nov 6;9(3):955-66. doi: 10.1016/j.celrep.2014.09.056. Epub 2014 Oct 30. PubMed PMID: 25437552; PubMed Central PMCID: PMC4488849.

4: Kawabe S, Yokoyama Y. Novel isoforms of heat shock transcription factor 1 are induced by hypoxia in the Pacific oyster Crassostrea gigas. J Exp Zool A Ecol Genet Physiol. 2011 Aug 1;315(7):394-407. doi: 10.1002/jez.685. Epub 2011 Mar 31. PubMed PMID: 21455948.

5: Neef DW, Turski ML, Thiele DJ. Modulation of heat shock transcription factor 1 as a therapeutic target for small molecule intervention in neurodegenerative disease. PLoS Biol. 2010 Jan 19;8(1):e1000291. doi: 10.1371/journal.pbio.1000291. PubMed PMID: 20098725; PubMed Central PMCID: PMC2808216.

6: Ojima N, Yamashita M. Cloning and characterization of two distinct isoforms of rainbow trout heat shock factor 1. Evidence for heterotrimer formation. Eur J Biochem. 2004 Feb;271(4):703-12. PubMed PMID: 14764086.

7: Airaksinen S, Jokilehto T, Råbergh CM, Nikinmaa M. Heat- and cold-inducible regulation of HSP70 expression in zebrafish ZF4 cells. Comp Biochem Physiol B Biochem Mol Biol. 2003 Oct;136(2):275-82. PubMed PMID: 14529753.

8: Murtha JM, Keller ET. Characterization of the heat shock response in mature zebrafish (Danio rerio). Exp Gerontol. 2003 Jun;38(6):683-91. PubMed PMID: 12814804.

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EOS Med Chem, Medicinal Chemical is Big

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2018年5月4日星期五

GMP Manufacturer: Ivosidenib; AG-120 (CAS 1448347-49-6) and intermediates.

Ivosidenib; AG-120 (CAS 1448347-49-6) : HPLC99.2%, LCMS, NMR, ROS, MOA, COA is ok, stock more than 10G.

Ivosidenib; AG-120 (CAS 1448347-49-6) Intermeidates:

Original:MSX-130 4051-59-6 , stock more than 100g

Original:E6446 HCl 1345675-25-3, stock more than 100g

Original:R-IMPP 2133832-83-2, stock more than 100g

Original: S38093 free base 862896-30-8 , stock more than 100g

Original:HSF1A 1196723-93-9 , stock more than 100g

举报滥用情况

2016 China CPHI meet