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PHA-767491 hydrochloride

PHA-767491 hydrochloride

产品编号 T6940   CAS 942425-68-5
别名: CAY10572, PHA-767491, PHA767491 HCl, CAY-10572 hydrochloride

PHA-767491 hydrochloride (CAY-10572 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
PHA-767491 hydrochloride, CAS 942425-68-5
规格 价格/CNY 货期 数量
1 mg ¥ 185 现货
5 mg ¥ 413 现货
10 mg ¥ 578 现货
25 mg ¥ 938 现货
50 mg ¥ 1,330 现货
100 mg ¥ 2,160 现货
200 mg ¥ 3,220 现货
500 mg ¥ 5,170 现货
1 mL * 10 mM (in DMSO) ¥ 455 现货
其他形式的 PHA-767491 hydrochloride:
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
Venetoclax限时半价
产品目录号及名称: PHA-767491 hydrochloride (T6940)
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纯度: 99.92%
纯度: 99.63%
纯度: 98.69%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 PHA-767491 hydrochloride (CAY-10572 hydrochloride) 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.
靶点活性 CDC7:10 nM, CDK9:34 nM
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.
别名 CAY10572, PHA-767491, PHA767491 HCl, CAY-10572 hydrochloride
分子量 249.69
分子式 C12H12ClN3O
CAS No. 942425-68-5

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

H2O: 25 mg/mL (100 mM)

DMSO: 25 mg/mL (100 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 4.005 mL 20.0248 mL 40.0497 mL 100.1242 mL
5 mM 0.801 mL 4.005 mL 8.0099 mL 20.0248 mL
10 mM 0.4005 mL 2.0025 mL 4.005 mL 10.0124 mL
20 mM 0.2002 mL 1.0012 mL 2.0025 mL 5.0062 mL
50 mM 0.0801 mL 0.4005 mL 0.801 mL 2.0025 mL
100 mM 0.04 mL 0.2002 mL 0.4005 mL 1.0012 mL

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TargetMol Library Books参考文献

1. Montagnoli A, et al. Nat Chem Biol, 2008, 4(6), 357-365. 2. Yecies D, et al. Blood, 2010, 115(16), 3304-3313.
Stachyose tetrahydrate Diclofenac diethylamine BAY 11-7082 CPTH2 Didymin Oxypalmatine CDKI-73 Ziyuglycoside I

相关化合物库

该产品包含在如下化合物库中:
激酶抑制剂库 神经退行性疾病化合物库 抗癌活性化合物库 抑制剂库 抗癌药物库 药物功能重定位化合物库 抗癌临床化合物库 HIF-1化合物库 细胞重编程化合物库 抗癌细胞代谢库

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Keywords

PHA-767491 hydrochloride 942425-68-5 Apoptosis Cell Cycle/Checkpoint PI3K/Akt/mTOR signaling Stem Cells GSK-3 CDK PHA 767491 CAY10572 Hydrochloride inhibit CAY10572 PHA-767491 PHA767491 HCl Cyclin dependent kinase PHA767491 Hydrochloride PHA767491 hydrochloride CAY-10572 Hydrochloride PHA-767491 Hydrochloride PHA 767491 Hydrochloride Inhibitor CAY-10572 CAY-10572 hydrochloride CAY 10572 Hydrochloride PHA767491 PHA 767491 hydrochloride CAY 10572 inhibitor

 

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