GNE-317

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Chemical Structure| 1394076-92-6 同义名 : -
CAS号 : 1394076-92-6
货号 : A964728
分子式 : C19H22N6O3S
纯度 : 99%+
分子量 : 414.48
MDL号 : MFCD28900677
存储条件：

Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 18 mg/mL(43.43 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
生物活性
靶点

  • PI3K
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.41mL

0.48mL

0.24mL

12.06mL

2.41mL

1.21mL

24.13mL

4.83mL

2.41mL
参考文献

[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.