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 |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
Related CDK Products |
---|
PF-07224826
PF-07224826 is a CDK2/4/6 inhibitor. |
INCB123667
INCB123667 is a CDK2 inhibitor. |
Senexin B
Senexin B is a potent, orally active CDK8/19 inhibitor with Kd values of 140 nM and 80 nM for CDK8 and CDK19, respectively. |
Q901
Q901 is a CDK7 inhibitor for tumor-related studies. |
NUV-422
NUV-422 is a CDK2/4/6 inhibitor that can be used in studies related to malignant gliomas. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.