Powder: -20°C for 3 years | In solvent: -80°C for 1 year
PKI-179 is an orally bioavailable dual inhibitor of PI3K and mammalian target of rapamycin (mTOR). In an in vitro enzymatic assay, it potently inhibits PI3K (IC50s = 8, 24, 17, and 74 nM for isoforms α, β, δ, and γ, respectively), two common PI3Kα mutants, E545K and H1047R (IC50s = 14 and 11 nM, respectively), and mTOR (IC50 = 0.42 nM). PKI-179 is selective for PI3K and mTOR over a panel of 361 other kinases at IC50 values up to 50 μM, hERG (IC50 < 30 μM), and cytochrome P450 (CYP) isoforms (IC50s < 30 μM), but does have activity for CYP2C8 (IC50 = 3 μM). It inhibits proliferation through the Akt/mTOR signaling pathway in MDA-361 breast and PC3MM2 prostate cancer cell lines in vitro (IC50s = 22 and 29 nM, respectively) and inhibits tumor growth in an MDA-361 mouse xenograft model when used at a dose of 50 mg/kg.
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 1,220 | 5日内发货 | ||
5 mg | ¥ 2,350 | 5日内发货 | ||
25 mg | ¥ 8,160 | 6-8周 | ||
50 mg | ¥ 10,600 | 6-8周 | ||
100 mg | ¥ 16,500 | 6-8周 |
产品描述 | PKI-179 is an orally bioavailable dual inhibitor of PI3K and mammalian target of rapamycin (mTOR). In an in vitro enzymatic assay, it potently inhibits PI3K (IC50s = 8, 24, 17, and 74 nM for isoforms α, β, δ, and γ, respectively), two common PI3Kα mutants, E545K and H1047R (IC50s = 14 and 11 nM, respectively), and mTOR (IC50 = 0.42 nM). PKI-179 is selective for PI3K and mTOR over a panel of 361 other kinases at IC50 values up to 50 μM, hERG (IC50 > 30 μM), and cytochrome P450 (CYP) isoforms (IC50s > 30 μM), but does have activity for CYP2C8 (IC50 = 3 μM). It inhibits proliferation through the Akt/mTOR signaling pathway in MDA-361 breast and PC3MM2 prostate cancer cell lines in vitro (IC50s = 22 and 29 nM, respectively) and inhibits tumor growth in an MDA-361 mouse xenograft model when used at a dose of 50 mg/kg. |
靶点活性 | mTOR:0.42 nM (IC50), PI3Kγ:74 nM (IC50), H1047R:77 nM (IC50), PI3Kα:8 nM (IC50), E545K:14 nM (IC50), PI3Kβ:24 nM (IC50), PI3Kδ:77 nM (IC50) |
分子量 | 525 |
分子式 | C25H29ClN8O3 |
CAS No. | 1463510-35-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: Slightly soluble
DMF: 2 mg/mL
DMSO:PBS(pH 7.2) (1:3): 0.25 mg/mL
DMSO: 2.5 mg/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。
PKI-179 hydrochloride 1463510-35-1 PKI 179 Hydrochloride PKI179 hydrochloride PKI179 Hydrochloride PKI 179 hydrochloride PKI-179 Hydrochloride Inhibitor inhibitor inhibit