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CAS No.: 1033735-94-2

GNE-493 Catalog No. CSN17410

GNE-493 is a potent, selective, and orally available dual pan-PI3K/mTOR inhibitor with IC50s of 3.4/12/16/16/32 nM for PI3Kα/PI3Kβ/PI3Kγ/PI3Kδ/mTOR respectively.

规格	价格	促销价格	库存	数量

400-920-2911

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tech@csnpharm.cn

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400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述The phosphatidylinositol 3-kinase (PI3K)/AKT/mammalian target of the rapamycin (mTOR) signalling pathway is hyperactivated or altered in many cancer types and regulates a broad range of cellular processes including survival, proliferation, growth, metabolism, angiogenesis and metastasis^[2]. GNE-493 is a potent, selective, and orally available dual pan-PI3-kinase/mTOR (mammalian target of rapamycin) inhibitor with IC₅₀s of 3.4 nM, 12 nM, 16 nM, 16 nM and 32 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ and mTOR^[3]. To confirm and compare in vivo efficacy, mice bearing xenografts are dosed orally once daily with 10 mg/kg of GNE-493 for 21 continuous days. Similar to observations made in the PC3 prostate cancer xenograft model, 10 mg/kg of GNE-493 results in 73% tumor growth inhibition at day 21 when compared to vehicle control animals^[3].
参考文献

[1] Sutherlin DP, Sampath D, et al. Discovery of (thienopyrimidin-2-yl)aminopyrimidines as potent, selective, and orally available pan-PI3-kinase and dual pan-PI3-kinase/mTOR inhibitors for the treatment of cancer. J Med Chem. 2010 Feb 11;53(3):1086-97.
[2] Ersahin T, Tuncbag N, Cetin-Atalay R. The PI3K/AKT/mTOR interactive pathway. Mol Biosyst. 2015;11(7):1946-1954.
[3] Sutherlin DP, Sampath D, Berry M, et al. Discovery of (thienopyrimidin-2-yl)aminopyrimidines as potent, selective, and orally available pan-PI3-kinase and dual pan-PI3-kinase/mTOR inhibitors for the treatment of cancer. J Med Chem. 2010;53(3):1086-1097.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.6850 mL
- 13.4248 mL
- 26.8496 mL
- 5 mM
- 0.5370 mL
- 2.6850 mL
- 5.3699 mL
- 10 mM
- 0.2685 mL
- 1.3425 mL
- 2.6850 mL

技术信息

CAS号

1033735-94-2

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C17H20N6O2S

运输

蓝冰

分子量

372.44

别名

溶解度

DMSO	74.0 mg/mL (198.7 mM)
Water	Insoluble
Ethanol	1.0 mg/mL (2.7 mM)

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