Description
As a potent CDK inhibitor, SCH 727965 can inhibit CDK2, CDK5, CDK1, and CDK9 with IC50 of 1 nM, 1nM, 3 nM and 4 nM.
Storage
2 years at -20 centigrade
Molecular Formula
C21H28N6O2
Solubility
DSMO 79 mg/mL Water
In vitro
As a potent CDK inhibitor, SCH 727965 can inhibit CDK2, CDK5, CDK1, and CDK9 with IC50 of 1 nM, 1nM, 3 nM and 4 nM. SCH 727965 is a potent DNA replication inhibitor that blocked thymidine DNA incorporation in A2780 cells with an IC50 of 4 nM. SCH 727965 inhibits phosphorylation of the Rb tumor suppressor protein and induces accumulation of the p85 PARP caspase cleavage product.
In vivo
In A2780 tumors, SCH 727965 i.p. administration at 8, 16, 32, and 48 mg/kg daily for 10 days resulted in tumor inhibition by 70%, 70%, 89%, and 96%, respectively. Single agent therapy with SCH727965 (40 mg/kg i.p. twice weekly) for 4 weeks significantly reduced subcutaneous tumor growth in 10/10 (100%) of tested low-passage human pancreatic cancer xenografts.
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