计算溶液所需的质量、体积或浓度。
为什么选择此级别
，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
干燥,-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
PKI-179 hydrochloride is a potent and orally active dual PI3K/mTOR inhibitor, with IC 50 s of 8 nM, 24 nM, 74 nM, 77 nM, and 0.42 nM for PI3K-α , PI3K-β , PI3K-γ , PI3K-δ and mTOR , respectively. PKI-179 hydrochloride also exhibits activity over E545K and H1047R , with IC 50 s of 14 nM and 11 nM, respectively. PKI-179 hydrochloride shows anti-tumor activity in vivo
In Vitro
PKI-179 inhibits the cell proliferation, with IC 50 s of 22 nM and 29 nM for MDA361 and PC3 cells, respectively. PKI-179 shows inhibitory activity against a panel of 361 other kinases, hERG and cytochrome P450 (CYP) isoforms at concentrations up to >30 μM, but does have activity for CYP2C8 (IC 50 =3 μM). MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
PKI-179 (5-50 mg/kg; p.o. once daily for 40 days) inhibits the tumor growth and is well tolerated in nude mice bearing MDA-361 human breast cancer tumors . PKI-179 (50 mg/kg; p.o.) results in good inhibition of PI3K signaling in nude mice bearing MDA361 tumor xenografts . PKI-179 exhibits good oral bioavailability (98% in nude mouse, 46% in rat, 38% in monkey, and 61% in dog) and a high half-life (>60 min) . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Nude mice bearing MDA-361 human breast cancer tumors Dosage: 5, 10, 25, 50 mg/kg Administration: I.p. every 3 days for 4 weeks Result: Exhibited pronounced tumor growth arrest when dosed above 10 mg/kg. No significant weight loss of tested animals was observed for all different dosages.
IC50& Target:mTOR 0.42 nM (IC 50 ) PI3Kα 8 nM (IC 50 ) PI3Kβ 24 nM (IC 50 ) PI3Kγ 74 nM (IC 50 ) PI3Kδ 77 nM (IC 50 ) E545K 14 nM (IC 50 ) H1047R 77 nM (IC 50 )
规格
别名
PKI-179 盐酸盐
规格或纯度
10mM in DMSO
英文名称
PKI-179 hydrochloride
生化机理
PKI-179 盐酸盐是一种强效口服活性 PI3K/mTOR 双抑制剂，对 PI3K-α 、PI3K-β 、PI3K-γ 、PI3K-δ 和 mTOR 的 IC 50 s 分别为 8 nM、24 nM、74 nM、77 nM 和 0.42 nM。PKI-179 盐酸盐还对 E545K 和
储存条件
干燥,-80℃储存
运输条件
特低温运输
作用类型
抑制剂
名称和识别符
技术文档
高级数据
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
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溶液计算器
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