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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 |
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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. |
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溶解性：
Soluble in DMSO |
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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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| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
北京