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PHA-767491

Cat. No. M2322
PHA-767491 Structure
Synonym:

CAY10572

Size Price Availability Quantity
10mg USD 75 In stock
50mg USD 300 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 213.24
Formula C12H11N3O
CAS Number 845714-00-3
Purity >98%
Solubility DMSO 20 mg/mL
Storage at -20°C
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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: PHA-767491, CAY10572 supplier, CDK, inhibitors

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