Enitociclib | CDK9 inhibitor | Probechem Biochemicals

Chemical Structure : Enitociclib

CAS No.: 1610358-56-9

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Enitociclib ((+)-BAY 1251152, VIP152)

货号: PC-63127Not For Human Use, Lab Use Only.

Enitociclib ((±)-BAY-1251152) is a potent, highly specific P-TEFb/CDK9 inhibitor with IC50 of 3 nM. displays> 50-fold selectivity against other CDKs.

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10 mg	￥2980	In stock
25 mg	￥4880	In stock
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生物&药学活性

Enitociclib ((±)-BAY-1251152) is a potent, highly specific P-TEFb/CDK9 inhibitor with IC50 of 3 nM.
BAY-1251152 exhibits ex vivo potency (MOLM-13 cells, IC50=29 nM) and enhanced selectivity against CDK2, permeability, solubility, and no efflux.
BAY-1251152 has demonstrated IC50 of 19.06, 16.57 and 74.64 nM against HeLa, SiHa and OVCAR-3 cells, respectively.
BAY-1251152 is the only selective CDK9 inhibitor currently undergoing clinical trialsagainst advanced malignancies (NHL and solid tumors; NCT02635672).

物理化学性质&存储条件

分子量	404.436
分子式	C19H18F2N4O2S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20 °C 12 个月; 4°C 6 个月	配置液 -80 °C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(+)-5-Fluoro-4-(4-fluoro-2-methoxyphenyl)-N-[4-[(S-methylsulfonimidoyl)methyl]pyridin-2-yl]pyridin-2-amine

参考文献

1. Ulrich T. Luecking, et al. Abstract 984: Identification of potent and highly selective PTEFb inhibitor BAY 1251152 for the treatment of cancer: from p.o. to i.v. application via scaffold hops. DOI: 10.1158/1538-7445.

Enitociclib ((+)-BAY 1251152, VIP152)

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Enitociclib ((+)-BAY 1251152, VIP152)

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