GDC-0349CAS号： 1207360-89-1分子式： C24H32N6O3分子量： 452.55描述纯度储存/保存方法别名可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)参考文献
| 产品描述 | |
| 描述 |
GDC-0349是一种有效的，选择性的，ATP竞争性的mTOR抑制剂，Ki为3.8 nM，比作用于PI3Kα和其他266种激酶的抑制效果高790倍。GDC-0349作用于mTOR比作用于其他266种激酶及所有PI3K亚型的选择性高很多。 |
| 纯度 |
>98%
|
| 储存/保存方法 |
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
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| 基本信息 | |
| 别名 |
RG7603
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| 可溶性/溶解性 |
Ethanol :6 mg/mL (13.25 mM)
DMSO :84 mg/mL (185.6 mM) |
| 生物活性 | |
| 靶点 |
mTOR,PI3Kα
|
| In vitro(体外研究) |
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.
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| In vivo(体内研究) |
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).
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| 参考文献 | |
| 参考文献 |
Pyrimidoaminotropanes as potent, selective, and efficacious small molecule kinase inhibitors of the mammalian target of rapamycin (mTOR).
Estrada AA,et al. J Med Chem. 2013 Apr 11;56(7):3090-101. PMID: 分子结构图
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