PHA-767491 hydrochloride

产品编号: T6940 别名:

CAY10572,PHA767491 HCl,PHA-767491,CAY-10572 hydrochloride

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。

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PHA-767491 hydrochloride Chemical Structure

CAS：942425-68-5

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生物活性化学信息储存和溶解度信息参考文献引用文献

产品描述

PHA-767491 is an effective ATP-competitive dual Cdc7/CDK9 inhibitor (IC50: 10/34 nM). It has ~20-fold selectivity against GSK3-β and CDK1/2, 50-fold selectivity against CDK5 and MK2, 100-fold selectivity against CHK2 and PLK1.

体外活性

PHA-767491 inhibits proliferation of HCC1954 cells (IC50: 0.64 μM) and Colo-205 cells (IC50: 1.3 μM). PHA-767491 is effective DDK inhibitors in vitro (IC50: 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 line [2]. PHA-767491 (0-10 μM) time- and dose-dependently decreases glioblastoma cell viability (IC50: about 2.5 μM) for U87-MG and U251-MG cells.

体内活性

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

激酶实验

20 ng of purified human DDK is pre-incubated with increasing concentrations of each DDK inhibitor for 5 min. Then 10 μCi (γ)-32P ATP and 1.5 μM cold ATP are added in a buffer containing 50 mM Tris-HCl (pH 7.5), 10 mM MgCl2, and 1 mM DTT and incubated for 30 min at 30°C. The proteins are denatured in 1X Laemmli buffer at 100°C followed by SDS-PAGE and autoradiography on HyBlot CL film. Auto-phosphorylation of DDK is used as an indicator of its kinase activity. 32P-labeled bands are quantified using ImageJ and the IC50 values are calculated using GraphPad.

细胞实验

For assays in 96 well plates 2500 cells are plated per well. After 24 hours, cells are treated with small molecule inhibitors and incubated for 72 hours at 37°C. Subsequently the cells are lysed and the ATP content is measured as an indicator of metabolically active cells using the CellTiter-Glo assay. IC50 values are calculated using the GraphPad software. For assays in six-well plates, 100,000 cells are plated per well. After 24 hours, cells are treated with small molecule inhibitors and incubated for varying time points. Cells are trypsinized and a suspension is made in 5 mL of phosphate buffered saline. 30 μL of this suspension is mixed with 30 μL of CellTiter-Glo reagent followed by a 10-minute incubation at room temperature. Luminescence is measured using EnVision 2104 Multilabel Reader and BioTek Synergy Neo Microplate Reader.

Cas No.

942425-68-5

分子式

C12H12ClN3O

分子量

249.7

别名

CAY10572;PHA767491 HCl;PHA-767491;CAY-10572 hydrochloride;PHA-767491 hydrochloride

参考文献

[1]Yecies D, et al. Blood, 2010, 115(16), 3304-3313.[2]Montagnoli A, et al. Nat Chem Biol, 2008, 4(6), 357-365.

储存和溶解度

H2O:25 mg/mL (100 mM)
DMSO:25 mg/mL (100 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years

剂量换算 PHA-767491 hydrochloride 942425-68-5

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Keywords

PHA767491 PHA 767491 inhibit CAY10572 CAY-10572 PHA767491 HCl Cyclin dependent kinase CDK CAY 10572 PHA-767491 CAY-10572 hydrochloride PHA767491 hydrochloride Inhibitor Apoptosis PHA 767491 hydrochloride 942425-68-5

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PHA-767491 hydrochloride

CAY10572,PHA767491 HCl,PHA-767491,CAY-10572 hydrochloride

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