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GDC-0349
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。
GDC-0349图片
CAS NO:1207360-89-1
包装与价格:
包装价格(元)
1 mg询价
5 mg询价
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RG-7603
GDC0349 是一种ATP竞争性的选择性mTOR抑制剂,Ki值为 3.8 nM。它对 PI3Kα 和其他 266 种激酶的抑制作用是 790 倍,可抑制mTORC1和mTORC2复合体。

产品描述

GDC-0349 is a potent and selective ATP-competitive inhibitor of mTOR with Ki of 3.8 nM, 790-fold inhibitory effect against PI3Kα and other 266 kinases. Phase 1.

体外活性

GDC-0349 has remarkable selectivity over 266 kinases, including all isoforms of PI3K. GDC-0349 inhibits downstream markers of mTOR, including phospho-4EBP1 and phospho-Akt(S473) in an in vivo PK/PD study in mouse, consistent with an inhibition of both mTORC1 and mTORC2 complexes. [1]

体内活性

GDC-0349 demonstrates pathway modulation and dose-dependent efficacy in mouse xenograft cancer models. When dosed orally once daily in athymic mice in a MCF7-neo/Her2 tumor xenograft model (PI3K mutation), GDC-0349 inhibits tumor growth in a dose-dependent manner. It is also efficacious in other xenograft models, including PC3 (PTEN null) and 786-O (VHL mutant). [1]

Cas No.

1207360-89-1

分子式

C24H32N6O3

分子量

452.559

别名

RG-7603

储存和溶解度

H2O:<1 mgml
Ethanol:6 mg/mL (13.25 mM)
DMSO:84 mg/mL (185.6 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
 
 
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