Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
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 |
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: 25 mg/mL (100 mM)
DMSO: 4.62 mg/mL (18.48 mM), Sonication is recommended.
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 | |
H2O | 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 |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
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