S80010 |
LCL161 |
源葉(MedMol) | ≥99% |
- 提示:詳情請下載說明書。
- 產(chǎn)品描述: LCL161 is a IAP inhibitor which inhibits XIAP in HEK293 cell and cIAP1 in MDA-MB-231 cell with IC50s of 35 and 0.4 nM, respectively.
- 靶點(diǎn): IC50: 35 nM (XIAP, in HEK293 cell), 0.40 nM (cIAP1, in MDA-MB-231);IAP
- 體內(nèi)研究:
Tumor-bearing mice are treated with vehicle or LCL161 p.o. at a dose of 50 mg/kg/day, or SC-2001 p.o. at a dose of 10 mg/kg/day, 5 days a week, or in combination for the duration of the study. Tumor growth is significantly inhibited by co-treatment with SC2001 and LCL161 and tumor size in the co-treatment group is only one third of that of the control group at the end of the study. LCL161 is a first-in-class oral Smac mimetic shown to induce degradation of cIAP1 and cleavage of caspase 3 in mouse xenograft models
- 參考文獻(xiàn):
1. Maria Ahn, et al. Potent, Dual cIAP1/XIAP Antagonists Induce Apoptosis in a Melanoma Stem Cell Population. 2. Chen KF, et al. Inhibition of Bcl-2 improves effect of LCL161, a SMAC mimetic, in hepatocellular carcinoma cells. Biochem Pharmacol. 2012 Aug 1;84(3):268-77. 3. Dhuria S, et al. Time-dependent inhibition and induction of human cytochrome P4503A4/5 by an oral IAP antagonist, LCL161, in vitro and in vivo in healthy subjects. J Clin Pharmacol. 2013 Jun;53(6):642-53. 4. Infante JR, et al. Phase I dose-escalation study of LCL161, an oral inhibitor of apoptosis proteins inhibitor, in patients with advanced solid tumors. J Clin Oncol. 2014 Oct 1;32(28):3103-10.
- 溶解性: Soluble in DMSO
- 保存條件: -20℃
- 配置溶液濃度參考:
1mg 5mg 10mg 1 mM 1.997 ml 9.987 ml 19.975 ml 5 mM 0.399 ml 1.997 ml 3.995 ml 10 mM 0.2 ml 0.999 ml 1.997 ml 50 mM 0.04 ml 0.2 ml 0.399 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。
輸入產(chǎn)品批號:
本計算器可幫助您計算出特定溶液中溶質(zhì)的質(zhì)量、溶液濃度和體積之間的關(guān)系,公式為:
質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)