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CAS No.: 1394076-92-6

GNE-317 Catalog No. CSN17784

GNE-317 is a potent PI3K/mTOR inhibitor that can cross the blood–brain barrier and shows potent suppression of the PI3K pathway in the brain of mice with intact BBB.

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实验方案

技术信息

生物活性

描述GNE-317 is an optimized dual PI3K/mTOR inhibitor, which can cross the blood–brain barrier. Compared with the control group, a single oral dose of 50mg/kg GNE-317 significantly reduced pAkt, p4EBP1, and pS6 by 80%, 84%, and 92%, respectively, in the brain of normal mice at 1h post treatment. Oral administration of GNE-317 greatly inhibited GS2 brain tumor at 40mg/kg, daily for 6 weeks and U87 brain tumor at 40mg/kg, daily for 3 weeks, as well as prolonged survival of orthotopic GBM10 model^[2].
动物研究
剂量
Mice: 50 mg/kg^[2] (p.o.)

给药途径
p.o.
参考文献

动物研究
剂量	Mice: 50 mg/kg^[2] (p.o.)
给药途径	p.o.

[1] Salphati L, Heffron TP, et al. Targeting the PI3K pathway in the brain--efficacy of a PI3K inhibitor optimized to cross the blood-brain barrier. Clin Cancer Res. 2012 Nov 15;18(22):6239-48.
[2] Salphati L, Heffron TP, Alicke B, Nishimura M, Barck K, Carano RA, Cheong J, Edgar KA, Greve J, Kharbanda S, Koeppen H, Lau S, Lee LB, Pang J, Plise EG, Pokorny JL, Reslan HB, Sarkaria JN, Wallin JJ, Zhang X, Gould SE, Olivero AG, Phillips HS. Targeting the PI3K pathway in the brain--efficacy of a PI3K inhibitor optimized to cross the blood-brain barrier. Clin Cancer Res. 2012 Nov 15;18(22):6239-48. doi: 10.1158/1078-0432.CCR-12-0720. Epub 2012 Sep 19. PMID: 22992516.

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
- 2.4127 mL
- 12.0633 mL
- 24.1265 mL
- 5 mM
- 0.4825 mL
- 2.4127 mL
- 4.8253 mL
- 10 mM
- 0.2413 mL
- 1.2063 mL
- 2.4127 mL

技术信息

CAS号

1394076-92-6

储存条件

粉末: Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H22N6O3S

运输

蓝冰

分子量

414.48

别名

溶解度

DMSO	19.0 mg/mL (45.8 mM)
Water	insoluble

动物实验配方

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