S80065 |
WYE-354 |
源叶(MedMol) | ≥98% |
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- 产品描述: WYE-354 is an ATP-competitive mTOR inhibitor with an IC50 of 5 nM. WYE-354 also inhibits PI3Kα and PI3Kγ with IC50s of 1.89 μM and 7.37 μM, respectively. WYE-354 inhibits both mTORC1 and mTORC2. WYE-354 induces autophagy activation in vitro
- 靶点: mTOR:5 nM (IC50);mTORC1;mTORC2;PI3K alpha:1.89 μM (IC50);PI3K gamma:7.37 μM (IC50);Autophagy ;Apoptosis;PI3K;mTOR;Autophagy
- 体内研究:
The effect of Rapamycin and WYE-354 on tumor growth is evaluated in xenograft GBC tumor models. 2×106 or 5×106 cells of G-415 or TGBC2TKB, respectively, are xenotransplanted into NOD-SCID mice subcutaneously. When tumors reach an average volume of 100 mm3, the mice are treated either with Rapamycin or WYE354. Rapamycin is administered i.p. at a concentration of 10 mg/kg, daily for 5 days per week for 3 weeks, while WYE-354 is administrated at a daily i.p. dose of 50 mg/kg for 5 days. Mice are sacrificed 30 days after the initiation of the treatments and an autopsy is performed that include removal of the entire tumor area. Mice treated with WYE-354 exhibit 68.6% and 52.4% reduction in average tumor size (P<0.01; P<0.01), as well as 82.9% and 45.5% (P<0.01; ns) reduction in tumor weight, respectively
- 参考文献:
1. Yu K et al. Biochemical, cellular, and in vivo activity of novel ATP-competitive and selective inhibitors of the mammalian target of rapamycin. Cancer Res. 2009 Aug 1;69(15):6232-40. 2. Weber H, et al. Rapamycin and WYE-354 suppress human gallbladder cancer xenografts in mice. Oncotarget. 2015 Oct 13;6(31):31877-88. 3. Lijun Wang, et al. Autophagy inhibition sensitizes WYE-354-induced anti-colon cancer activity in vitro and in vivo. Tumour Biol. 2016 Sep;37(9):11743-11752.
- 溶解性: Soluble in DMSO
- 保存条件: -20℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 2.018 ml 10.09 ml 20.18 ml 5 mM 0.404 ml 2.018 ml 4.036 ml 10 mM 0.202 ml 1.009 ml 2.018 ml 50 mM 0.04 ml 0.202 ml 0.404 ml
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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)