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Chemical Structure : Crozbaciclib
CAS No.: 2099128-41-1
Catalog No.: 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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|---|---|---|---|
| 5 mg | $398 | In stock | |
| 10 mg | $598 | In stock | |
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| 100 mg | Get quote |
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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
| M.Wt | 488.587 | |
| Formula | C28H30F2N6 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| 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 |
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1. Lei Yin, et al. Eur J Med Chem. 2018 Jan 20;144:1-28.
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