PHA-767491 hydrochloride 是一种 Cdc7-Dbf4 (DDK)/Cdk9 的双重抑制剂，IC₅₀ 值分别为 10 nM 和 34 nM。

PHA-767491 hydrochloride is a dual Cdc7/Cdk9 inhibitor, with IC 50 s of 10 nM and 34 nM, respectively.

Solid

CDK9 34 nM (IC50) CDK2 240 nM (IC50

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 hydrochlo

PHA-767491 decreases Chk1 phosphorylation and increases in situ cell apoptosis in tumor tissues sectioned from nude mice HCC xenografts. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

[1]. Sasi NK, et al. The potent Cdc7-Dbf4 (DDK) kinase inhibitor XL413 has limited activity in many cancer cell lines and discovery of potential new DDK inhibitor scaffolds. PLoS One. 2014 Nov 20;9(11):e113300.
[2]. Li W, et al. Dual Inhibition of Cdc7 and Cdk9 by PHA-767491 Suppresses Hepatocarcinoma Synergistically with 5-Fluorouracil. Curr Cancer Drug Targets. 2015;15(3):196-204.

In Vitro: H₂O : 50 mg/mL (200.24 mM; Need ultrasonic)DMSO : 17.33 mg/mL (69.40 mM; Need ultrasonic and warming)配制储备液