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PHA-767491

Cat. No. M2322
PHA-767491 Structure
Synonym:

CAY10572

Size Price Availability Quantity
5mg USD 50  USD50 In stock
10mg USD 70  USD70 In stock
50mg USD 250  USD250 In stock
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Quality Control & Documentation
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.

Chemical Information
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
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Elisa Rojas-Prats, et al. Increasing Brain Permeability of PHA-767491, a Cell Division Cycle 7 Kinase Inhibitor, with Biodegradable Polymeric Nanoparticles

[2] Yu-Han Chung, et al. Targeting Inflammation, PHA-767491 Shows a Broad Spectrum in Protein Aggregation Diseases

[3] Eimear O' Reilly, et al. Repression of Mcl-1 expression by the CDC7/CDK9 inhibitor PHA-767491 overcomes bone marrow stroma-mediated drug resistance in AML

[4] Hsiu-Yu Liu, et al. Repurposing of the CDK inhibitor PHA-767491 as a NRF2 inhibitor drug candidate for cancer therapy via redox modulation

[5] Wei Li, et al. Dual Inhibition of Cdc7 and Cdk9 by PHA-767491 Suppresses Hepatocarcinoma Synergistically with 5-Fluorouracil

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  Catalog
Abmole Inhibitor Catalog




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


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