BMS695735 - CAS 1054315-48-8
Catalog number:
1054315-48-8
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C26H31ClFN7O
Molecular Weight:
512.02
COA:
Inquire
Targets:
IGF-1R
Description:
BMS695735 is a benzimidazole inhibitor of the insulin-like growth factor-1 receptor. It was also found to have potent CYP3A4 inhibition. It has broad spectrum in vivo antitumor activity.
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Purity:
95%
Appearance:
Solid powder
Synonyms:
2(1H)-Pyridinone, 4-((2-(4-chloro-1H-pyrazol-1-yl)ethyl)amino)-3-(5-(1-(3-fluoropropyl)-4-piperidinyl)-7-methyl-1H-benzimidazol-2-yl)-;(3Z)-4-[2-(4-chloropyrazol-1-yl)ethylamino]-3-[6-[1-(3-fluoropropyl)piperidin-4-yl]-4-methyl-1,3-dihydrobenzimidazol-2-ylidene]pyridin-2-one;BMS-695735
Solubility:
10 mM in DMSO
Storage:
-20°C Freezer
MSDS:
Inquire
Application:
BMS695735 has broad spectrum antitumor activity.
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Quantity:
Milligrams-Grams
Density:
1.41±0.1 g/cm3 | Condition: Temp: 20 °C Press: 760 Torr
InChIKey:
KPIXLYXGTRJJMP-BZZOAKBMSA-N
InChI:
InChI=1S/C26H31ClFN7O/c1-17-13-19(18-4-10-34(11-5-18)9-2-6-28)14-22-24(17)33-25(32-22)23-21(3-7-30-26(23)36)29-8-12-35-16-20(27)15-31-35/h3,7,13-16,18,29,32-33H,2,4-6,8-12H2,1H3/b25-23-
Canonical SMILES:
CC1=C2C(=CC(=C1)C3CCN(CC3)CCCF)NC(=C4C(=CC=NC4=O)NCCN5C=C(C=N5)Cl)N2
1.Discovery and evaluation of 4-(2-(4-chloro-1H-pyrazol-1-yl)ethylamino)-3-(6-(1-(3-fluoropropyl)piperidin-4-yl)-4-methyl-1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-one (BMS-695735), an orally efficacious inhibitor of insulin-like growth factor-1 receptor kinase with broad spectrum in vivo antitumor activity.
Velaparthi U1, Wittman M, Liu P, Carboni JM, Lee FY, Attar R, Balimane P, Clarke W, Sinz MW, Hurlburt W, Patel K, Discenza L, Kim S, Gottardis M, Greer A, Li A, Saulnier M, Yang Z, Zimmermann K, Trainor G, Vyas D. J Med Chem. 2008 Oct 9;51(19):5897-900. doi: 10.1021/jm800832q. Epub 2008 Sep 3.
We previously reported that 1 (BMS-536924), a benzimidazole inhibitor of the insulin-like growth factor-1 receptor, had demonstrated in vivo antitumor activity. This lead compound was found to have potent CYP3A4 inhibition, CYP3A4 induction mediated by PXR transactivation, poor aqueous solubility, and high plasma protein binding. Herein we disclose the evolution of this chemotype to address these issues. This effort led to 10 (BMS-695735), which exhibits improved ADME properties, a low risk for drug-drug interactions, and in vivo efficacy in multiple xenograft models.
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CAS 1054315-48-8 BMS695735

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