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Crozbaciclib

Chemical Structure : Crozbaciclib

CAS No.: 2099128-41-1

Crozbaciclib

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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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

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

Physicochemical Properties

M.Wt 488.587
Formula C28H30F2N6
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
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

References

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

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