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PKI-179(hydrochloride)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
PKI-179(hydrochloride)图片
CAS NO:1463510-35-1
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议

产品介绍
PKI-179 (hydrochloride) 是一种有效且具有口服活性的双重 PI3K/mTOR 抑制剂,对 PI3K-α、PI3K-β、PI3K-γ、PI3K 的 IC50 分别为 8 nM、24 nM、74 nM、77 nM 和 0.42 nM -δ 和 mTOR,分别。 PKI-179 (hydrochloride) 也表现出对 E545K 和 H1047R 的活性,IC50 分别为 14 nM 和 11 nM。 PKI-179(盐酸盐)在体内显示出抗肿瘤活性。
Cas No.1463510-35-1
Canonical SMILESO=C(NC1=CC=C(C2=NC(N3CCOCC3)=NC(N4C5COCC4CC5)=N2)C=C1)NC6=CC=NC=C6.Cl
分子式C25H28N8O3•HCl
分子量525
溶解度DMF: 2 mg/ml,DMSO: 2.5 mg/ml,DMSO:PBS(pH 7.2) (1:3): 0.25 mg/ml,Ethanol: slightly soluble
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
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.