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产品描述 |
Taselisib, also known as GDC0032 or RG7606, is a selective, potent, orally bioavailable inhibitor of PI3Ka with a Ki = 0.2nM, and with reduced inhibitory activity against PI3Kβ. This selectivity profile, and excellent pharmacokinetic and pharmaceutical properties, allowed for greater efficacy in vivo at the maximum tolerated dose relative to a pan Class I PI3K inhibitor in PIK3CA mutant xenografts. Notably, GDC-0032 preferentially inhibited PIK3CA mutant cells relative to cells with wild-type PI3K. GDC-0032 potently inhibits signal transduction downstream of PI3K and induces apoptosis at low concentrations in breast cancer cell lines and xenograft models that harbor PIK3CA mutations. |
化学结构 |
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化学名称 |
2-(4-(2-(1-isopropyl-3-methyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)-1H-pyrazol-1-yl)-2-methylpropanamide |
SMILES Code |
CC(C)(N1N=CC(C2=CC=C3C4=NC(C5=NC(C)=NN5C(C)C)=CN4CCOC3=C2)=C1)C(N)=O |
基本信息 |
产品编号:XM176 产品名称:Taselisib (GDC0032) 别名:GDC0032; GDC0032; GDC 0032; RG7604; RG7604; RG 7604; Taselisib. CAS#:1282512-48-4 分子式:C24H28N8O2 精确分子量:460.23352 分子量:460.53
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物化性质 |
外观: 固体粉末
纯度: >98%
运输信息: 非危险化学品,适于常温或冰袋运输。
储存条件: 低温,干燥,避光。
溶解性: 溶于DMSO, 不溶于水
储存期限:3年 -20℃固体储存
2 年 -80℃ 溶液储存 |
该产品只供科研使用,不能给病人提供。
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