PHA-767491

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

PHA-767491 是一种有效的 ATP 竞争性双重 Cdc7/CDK9 抑制剂，IC50 分别为 10 nM 和 34 nM。

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

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.

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

CAY10572

Others

Other Targets

Cdc7| CDK1| CDK2| CDK9| GSK-3β

Cancer

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845714-00-3

213.24

C12H11N3O

>98% (HPLC)

——

C1CNC(=O)c2c1[nH]c(c2)c1ccncc1

——

(-20℃)

With Ice Pack

≥ 2 years