| 產(chǎn)品描述： | Torin 1 is a potent inhibitor of mTOR with an IC50 of 3 nM. Torin 1 inhibits both mTORC1/2 complexes with IC50 values between 2 and 10 nM. Torin 1 is an effective inducer of autophagy. |
| 靶點(diǎn)： |
mTORC1:2-10 nM (IC50);mTORC2:2-10 nM (IC50);mTOR:3 nM (IC50);DNA-PK:1 μM (IC50);PI3K-α:1.8 μM (IC50);ATM:0.6 μM (IC50);hVps34:3 μM (IC50);Autophagy;DNA-PK;PI3K;mTOR;Autophagy |
| 體內(nèi)研究： |
Torin1 (20 mg/kg, i.p.) is efficacious in a U87MG xenograft model, and demonstrates good pharmacodynamic inhibition of downstream effectors of mTOR in tumor and peripheral tissues |
| 參考文獻(xiàn)： |
1. Thoreen CC, et al, An ATP-competitive mammalian target of rapamycin inhibitor reveals rapamycin-resistant functions of mTORC1. J Biol Chem, 2009, 284(12), 8023-8032. 2. Liu Q, et al. Discovery of 1-(4-(4-propionylpiperazin-1-yl)-3-(trifluoromethyl)phenyl)-9-(quinolin-3-yl)benzo[h][1,6]naphthyridin-2(1H)-one as a highly potent, selective mammalian target of rapamycin (mTOR) inhibitor for the treatment of cancer. J Med Che 3. Bi C, et al. Inhibition of 4EBP phosphorylation mediates the cytotoxic effect of mechanistic target of rapamycin kinase inhibitors in aggressive B-cell lymphomas. Haematologica. 2017 Apr;102(4):755-764. 4. Brandt M, et al. mTORC1 Inactivation Promotes Colitis-Induced Colorectal Cancer but Protects from APC Loss-Dependent Tumorigenesis. Cell Metab. 2018 Jan 9;27(1):118-135.e8. |
| 溶解性： |
DMSO : 2 mg/mL (3.29 mM; ultrasonic and warming and heat to 60°C) |
| 保存條件： |
-20℃ |
| 配置溶液濃度參考： |
|
1mg |
5mg |
10mg |
| 1 mM |
1.646 ml |
8.229 ml |
16.458 ml |
| 5 mM |
0.329 ml |
1.646 ml |
3.292 ml |
| 10 mM |
0.165 ml |
0.823 ml |
1.646 ml |
| 50 mM |
0.033 ml |
0.165 ml |
0.329 ml |
|
| 注意： |
部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。 |
上海工商
危險(xiǎn)品化學(xué)品經(jīng)營(yíng)許可證（不帶存儲(chǔ)）
營(yíng)業(yè)執(zhí)照(三證合一)
北京