PHA-767491 is a dualCdc7/Cdk9inhibitor, withIC₅₀s of 10 nM and 34 nM, respectively.

PHA-767491 inhibits proliferation in both cell lines with an IC₅₀of 0.64 μM in HCC1954 cells and 1.3 μM in Colo-205 cells. PHA-767491 is effective DDK inhibitors in vitro, with IC₅₀values of 18.6 nM. PHA-767491 (2 μM) completely abolishes Mcm2 phosphorylation by 24 hours in HCC1954 cells^[1]. 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^[2]. PHA-767491 (0-10 μM) decreases glioblastoma cell viability in a time- and dose-dependent fashion, with IC₅₀of 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^[3].

PHA-767491 decreases Chk1 phosphorylation and increases in situ cell apoptosis in tumor tissues sectioned from nude mice HCC xenografts^[2].

213.24

C₁₂H₁₁N₃O

845714-00-3

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.