PHA 793887 Inhibitor Cas 718630-59-2 Against CDK2 CDK1 CDK4
PHA 793887 Inhibitor Cas 718630-59-2 Against CDK2 CDK1 CDK4
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Chemical Information
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Product name:PHA-793887 |
Purity:98% min |
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CAS NO:718630-59-2 |
Solubility:DMSO50 mg/mL (138.32 mM) |
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Molecular Formula:C19H31N5O2 |
Package:Package according to customer requirements |
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Molecular Weight:361.482 |
Storage:Store at -20℃ |
Quality control
COA
Remarks
PHA-793887 is an inhibitor of multiple cyclin dependent kinases (CDK) with activity against CDK2, CDK1 and CDK4. PHA-793887 was cytotoxic for leukemic cell lines in vitro, with IC(50) ranging from 0.3 to 7 microM. In colony assays PHA-793887 showed very high activity against leukemia cell lines, with an IC(50) <0.1 microM indicating that it has efficient and prolonged antiproliferative activity. PHA-793887 induced cell-cycle arrest, inhibited Rb and nucleophosmin phosphorylation. PHA-793887 has promising therapeutic activity against acute leukemias in vitro and in vivo.
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References
[1].Locatelli G, et al. Transcriptional analysis of an E2F gene signature as a biomarker of activity of the cyclin-dependent kinase inhibitor PHA-793887 in tumor and skin biopsies from a phase I clinical study. Mol Cancer Ther. 2010 May;9(5):1265-73.
[2].Massard C, et al. A first in man, phase I dose-escalation study of PHA-793887, an inhibitor of multiple cyclin-dependent kinases (CD
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