Powder: -20°C for 3 years | In solvent: -80°C for 1 year
PHA-793887 是一种ATP 竞争性的CDK 抑制剂,可抑制 Cdk2、Cdk1、Cdk4 和 Cdk9 的活性,IC50值分别为 8 nM、60 nM、62 nM 和 138 nM,同时可抑制糖原合酶激酶 3β,IC50值为 79 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 289 | 现货 | ||
2 mg | ¥ 413 | 现货 | ||
5 mg | ¥ 745 | 现货 | ||
10 mg | ¥ 1,180 | 现货 | ||
25 mg | ¥ 2,250 | 现货 | ||
50 mg | ¥ 3,580 | 现货 | ||
100 mg | ¥ 5,130 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 592 | 现货 |
产品描述 | PHA-793887 has been used in trials studying the treatment of Advanced/Metastatic Solid Tumors. |
靶点活性 | CDK5-p25:5 nM, CDK2-CyclinE:8 nM, CDK7-CyclinH:10 nM, CDK2-CyclinA:8 nM, CDK1-CyclinB:60 nM |
体外活性 | 20 mg/kg PHA-793887对携带K562和HL60细胞的移植瘤模型,原代白血病扩散细胞模型和复发Philadelphia-阳性急性淋巴性白血病患者高负荷播散性ALL-2模型有效.PHA-793887(10-30 mg/kg)在人卵巢A2780,结肠HCT-116和胰腺BX-PC3癌异种移植模型中显示出良好的功效. |
体内活性 | PHA-793887诱导细胞周期停滞,抑制Rb和核磷酸磷酸化,0.2-1 μM时调节细胞周期蛋白E和cdc6表达,5 μM时诱导凋亡。PHA-793887对白血病细胞系(包括K562,KU812,KCL22和TOM1)具有细胞毒性,IC50为0.3-7 μM,但对正常未刺激的外周血单个核细胞或CD34 +造血干细胞没有细胞毒性。PHA-793887作用于白血病细胞系具有高活性,IC50< 0.1 μM。 PHA-793887抑制许多肿瘤细胞系(包括A2780,HCT-116,COLO-205,C-433,DU-145,A375,PC3,MCF-7和BX-PC3)的细胞增殖,IC50为88 nM- 3.4 μM。 |
激酶实验 | CDK Kinase Assay: The biochemical activity of compounds is determined by incubation with specific enzymes and substrates, followed by quantitation of the phosphorylated product. PHA-793887 (1.5 nM–10 μM) is incubated for 30?90 min at room temperature in the presence of ATP/33P-γ-ATP mix, substrate, and the specific enzyme (0.7?100 nM) in a final volume of 30 μL of kinase buffer, using 96 U bottom plates. After incubation, the reaction is stopped and the phosphorylated substrate is separated from nonincorporated radioactive ATP using SPA beads, Dowex resin, or Multiscreen phosphocellulose filter as follows: (1) For SPA Assays. The reaction is stopped by the addition of 100 μL of PBS + 32 mM EDTA + 0.1% Triton X-100 + 500 μM ATP, containing 1 mg of streptavidin-coated SPA beads. After 20 min of incubation for substrate capture, 100 μL of the reaction mixture is transferred into Optiplate 96-well plates containing 100 μL of 5 M CsCl, left to stand for 4 hours to allow stratification of beads to the top of the plate, and counted using TopCount to measure substrate-incorporated phosphate. (2) For Dowex Resin Assay. An amount of 150 μL of resin/formate, pH 3.00, is added to stop the reaction and capture unreacted 33P-γ-ATP, separating it from the phosphorylated substrate in solution. After 60 min of rest, 50 μL of supernatant is transferred to Optiplate 96-well plates. After the additon of 150 μL of Microscint 40, the radioactivity is counted in the TopCount. (3) For Multiscreen Assay. The reaction is stopped with the addition of 10 μL of EDTA (150 mM). An amount of 100 μL is transferred to a MultiScreen plate to allow substrate binding to phosphocellulose filter. Plates are then washed three times with 100 μL of H2PO4 (75 mM) filtered by a MultiScreen filtration system, and dried. After the additon of 100 μL of Microscint 0, radioactivity is counted in the TopCount. IC50 values are obtained by nonlinear regression analysis. |
细胞实验 | Cells are seeded into 96- or 384-wells plates at final concentration ranging from 1 × 104 to 3 × 104 per cm2. After 24 hours, cells are treated using serial dilution of PHA-793887. At 72 hours after the treatment, the amount of cells are evaluated using the CellTiter-Glo assay. IC50 values are calculated using a sygmoidal fitt(Only for Reference) |
别名 | PHA 793887, PHA793887 |
分子量 | 361.48 |
分子式 | C19H31N5O2 |
CAS No. | 718630-59-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 67 mg/mL (185.3 mM)
DMSO: 67 mg/mL (185.3 mM)
H2O: < 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 |
Ethanol / DMSO | 1 mM | 2.7664 mL | 13.832 mL | 27.664 mL | 69.1601 mL |
5 mM | 0.5533 mL | 2.7664 mL | 5.5328 mL | 13.832 mL | |
10 mM | 0.2766 mL | 1.3832 mL | 2.7664 mL | 6.916 mL | |
20 mM | 0.1383 mL | 0.6916 mL | 1.3832 mL | 3.458 mL | |
50 mM | 0.0553 mL | 0.2766 mL | 0.5533 mL | 1.3832 mL | |
100 mM | 0.0277 mL | 0.1383 mL | 0.2766 mL | 0.6916 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-793887 718630-59-2 Apoptosis Cell Cycle/Checkpoint CDK PHA 793887 Inhibitor inhibit PHA793887 Cyclin dependent kinase inhibitor