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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-Cyclin-dependent Kinase (CDK)-Crozbaciclib
Crozbaciclib

Chemical Structure : Crozbaciclib

CAS No.: 2099128-41-1

Crozbaciclib

货号: PC-49130Not For Human Use, Lab Use Only.

Crozbaciclib is a highly potent, selective, blood-brain barrier (BBB) permeable CDK4/6 inhibitor with IC50 values of 3 nM and 1 nM against CDK4/cyclin D1 and CDK6/cyclin D3, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Crozbaciclib is a highly potent, selective, blood-brain barrier (BBB) permeable CDK4/6 inhibitor with IC50 values of 3 nM and 1 nM against CDK4/cyclin D1 and CDK6/cyclin D3, respectively.
Crozbaciclib exhibits a favorable pharmacological profile and significant penetration of the BBB with the Kp value of 4.10 and the Kp,uu value of 0.23 in mice after an oral dose of 10 mg/kg.
Crozbaciclib exhibits significant tumor growth inhibition values ranging from 62% to 99% for doses ranging from 3.125 to 50 mg/kg in orthotopic xenograft mouse model of glioblastoma multiforme (GBM), with no significant body weight loss

物理化学性质&存储条件

分子量 488.587
分子式 C28H30F2N6
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-(7'-fluoro-2'-methylspiro[cyclopentane-1,3'-indol]-5'-yl)-N-(5-(1-methylpiperidin-4-yl)pyridin-2-yl)pyrimidin-2-amine

参考文献

1. Lei Yin, et al. Eur J Med Chem. 2018 Jan 20;144:1-28.

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