Powder: -20°C for 3 years | In solvent: -80°C for 1 year
PHA-767491 (CAY10572) 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。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 312 | 现货 | ||
5 mg | ¥ 443 | 现货 | ||
10 mg | ¥ 616 | 现货 | ||
25 mg | ¥ 1,320 | 现货 | ||
50 mg | ¥ 2,290 | 现货 | ||
100 mg | ¥ 3,390 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 443 | 现货 |
产品描述 | PHA-767491 (CAY10572) is a potent ATP-competitive dual Cdc7/CDK9 inhibitor with IC50 of 10 nM and 34 nM, respectively. |
靶点活性 | CDC7:10 nM, CDK9:34 nM |
体外活性 | PHA-767491降低Chk1磷酸化并增加从裸鼠HCC异种移植物切片的肿瘤组织中的原位细胞凋亡. |
体内活性 | PHA-767491抑制两种细胞系的增殖,在HCC1954细胞中的IC50为0.64 μM,在Colo-205细胞中的IC50为1.3 μM。PHA-767491(2 μM)在HCC1954细胞中24小时完全消除Mcm2磷酸化。PHA-767491与5-FU联用对HCC细胞表现出更强的细胞毒性并诱导显著的凋亡,表现为显著增加的胱天蛋白酶3激活和聚(ADP-核糖)聚合酶片段化。 PHA-767491直接抵消5-FU诱导的Chk1的磷酸化并降低抗凋亡蛋白髓性白血病细胞1ine的表达。 PHA-767491(0-10 μM)以时间和剂量依赖方式降低成胶质细胞瘤细胞活力,U87-MG和U251-MG细胞的IC50约为2.5 μM。 |
激酶实验 | 20 ng of purified human DDK, together with increasing concentrations of each DDK inhibitor is pre-incubated 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. DDK kinase activity is indicated by Auto-phosphorylation of DDK. 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, PHA767491, PHA 767491 |
分子量 | 213.24 |
分子式 | C12H11N3O |
CAS No. | 845714-00-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 24 mg/mL (112.54 mM)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 4.6896 mL | 23.4478 mL | 46.8955 mL | 117.2388 mL |
5 mM | 0.9379 mL | 4.6896 mL | 9.3791 mL | 23.4478 mL | |
10 mM | 0.469 mL | 2.3448 mL | 4.6896 mL | 11.7239 mL | |
20 mM | 0.2345 mL | 1.1724 mL | 2.3448 mL | 5.8619 mL | |
50 mM | 0.0938 mL | 0.469 mL | 0.9379 mL | 2.3448 mL | |
100 mM | 0.0469 mL | 0.2345 mL | 0.469 mL | 1.1724 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。
PHA-767491 845714-00-3 Cell Cycle/Checkpoint GPCR/G Protein PI3K/Akt/mTOR signaling Stem Cells cholecystokinin GSK-3 CDK CAY10572 PHA767491 Cyclin dependent kinase CAY-10572 CAY 10572 inhibit Inhibitor PHA 767491 inhibitor