PHA-767491

SKU: orb1221736

Description

PHA-767491 is a potent ATP-competitive dual Cdc7/CDK9 inhibitor with IC50 of 10 nM and 34 nM, respectively.

Research Area

Metabolism Research

Key Properties

• CAS Number: 845714-00-3
• MW: 213.24
• Purity: >98% (HPLC)
• Formula: C₁₂H₁₁N₃O
• SMILES: C1CNC(=O)c2c1[nH]c(c2)c1ccncc1
• Target: Cdc7| CDK1| CDK2| CDK9| GSK-3β

Bioactivity

• In Vivo:
  PHA-767491 decreases Chk1 phosphorylation and increases in situ cell apoptosis in tumor tissues sectioned from nude mice HCC xenografts.
• In Vitro:
  PHA-767491 inhibits proliferation in both cell lines with an IC50 of 0.64 μM in HCC1954 cells and 1.3 μM in Colo-205 cells. PHA-767491 is effective DDK inhibitors in vitro, with IC50 values of 18.6 nM. PHA-767491 (2 μM) completely abolishes Mcm2 phosphorylation by 24 hours in HCC1954 cells. PHA-767491 in combination with 5-FU exhibits much stronger cytotoxicity and induces significant apoptosis manifested by remarkably increased caspase 3 activation and poly(ADP-Ribose) polymerase fragmentation in HCC cells. PHA-767491 directly counteracts the 5-FU-induced phosphorylation of Chk1 and decreases the expression of the anti-apoptotic protein myeloid leukemia cell 1ine. PHA-767491 (0-10 μM) decreases glioblastoma cell viability in a time- and dose-dependent fashion, with IC50 of approximately 2.5 μM for U87-MG and U251-MG cells. PHA-767491 hydrochloride induces apoptosis in glioblastoma cells, suppresses glioblastoma cell proliferation, cell migration and cell invasion.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CAY10572

Quick Database Links

Gene Symbol

Cdc7| CDK1| CDK2| CDK9| GSK-3β