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PHA-767491 is a potent, ATP-competitive dual cdk7/cdk9 inhibitor with IC50 of 10 and 34 nM for cdk7 and CDK9, respectively. PHA-767491 blocks the activity of mitogen-activated protein kinase-activated protein kinase-2 (MK-2) with anIC50 of 171 nM. PHA-767491 inhibits DNA synthesis and replication and influences the phosphorylation of the replicative DNA helicase at cdk7-dependent phosphorylation sites. PHA-767491 does not induce a sustained DNA damage response. PHA-767491 suppresses the proliferation of cell in a variety of human cell lines with IC50 values ranging from 0.86 to 5.87 μM. PHA-767491 induces apoptosis in a p53-independent manner in vivo. Treatment with PHA-76749 leads to apoptotic cell death in multiple cancer cell types and tumor growth inhibition in preclinical cancer models.
| Molecular Weight | 213.24 |
| Formula | C12H11N3O |
| CAS Number | 845714-00-3 |
| Solubility (25°C) | DMSO 20 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related CDK Products |
|---|
| (E/Z)-Zotiraciclib citrate
(E/Z)-Zotiraciclib citrate is a potent CDK2, JAK2, and FLT3 inhibitor. |
| Abemaciclib metabolites M2
Abemaciclib metabolite M2 (LSN2839567) is a metabolite of Abemaciclib, acts as a potent CDK4 and CDK6 inhibitor, with IC50 values of 1.2 and 1.3 nM, respectively. |
| CDK9-IN-1
CDK9-IN-1 is a novel, selective CDK9 inhibitor, with an IC50 of 39 nM for CDK9/CycT1, it can be used for the research of HIV infection. |
| XO44
XO44 (PF-6808472) is a broad-spectrum covalent kinase probe. |
| ML 315
ML 315 is a selective dual inhibitor of CDK and DYRK with IC50s of 68 nM and 282 nM, respectively. |
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Products are for research use only. Not for human use. We do not sell to patients.
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