Powder: -20°C for 3 years | In solvent: -80°C for 1 year
MTI-31 (LXI-15029) 是口服有效的,高度选择性的mTORC1和mTORC2抑制剂,对 mTOR 的Kd 为 0.20 nM,IC50为 39 nM。MTI-31可用于乳腺癌的研究。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 2,330 | 现货 | ||
5 mg | ¥ 5,630 | 现货 | ||
10 mg | ¥ 7,880 | 现货 | ||
25 mg | ¥ 11,600 | 现货 | ||
50 mg | ¥ 15,700 | 现货 | ||
100 mg | ¥ 21,200 | 现货 |
产品描述 | MTI-31 (LXI-15029) is a potent, orally active and highly selective inhibitor of mTORC1 and mTORC2. MTI-31 is selective for mTOR (Kd: 0.20 nM) versus PIK3CA, PIK3CB and PIK3G with >5,000 fold selectivity in mTOR binding assays. MTI-31 shows an IC50 of 39 nM for mTOR in LANCE assay of mTOR substrate phosphorylation with 100 μM ATP[1]. |
靶点活性 | mTOR:0.2 nM(Kd) |
体外活性 | MTI-31 (0.01-100 μM) elicits a potent and more substantial inhibition of cell growth than that of Rapamycin[1]. Treatment with MTI-31 for 6 h demonstrates a dose-dependent inhibition of both the mTORC1 substrates P-S6K1(T389), P-S6(S235/6), P-4EBP1(T70) and mTORC2 substrate P-AKT(S473), achieving 50% inhibition at ≤0.12 μM in three representative tumor cell lines harboring mTOR pathway dysregulation (786-O renal, U87MG glioma and MDA-MB-453 breast)[1]. MTI-31-induced apoptosis requires mTORC2-regulated Bim- and GSK3 activity[1]. |
体内活性 | MTI-31(5-40 mg/kg; orally) is efficacious in several tumor models harboring HER2+/PIK3CAmut and/or PTEN-deficiency exemplified by MDA-MB-453 and 786-O[1]. Treatment of tumor bearing nude mice with orally administered MTI-31 inhibits growth of H1975 tumors (25 mg/kg/d; orally) or U87MG tumors (30 mg/kg/d; orally)[2]. |
别名 | MTI-31, LXI-15029 |
分子量 | 474.55 |
分子式 | C26H30N6O3 |
CAS No. | 1567915-38-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 8.33 mg/mL (17.55 mM), Sonication and heating to 60℃ are recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.1073 mL | 10.5363 mL | 21.0726 mL | 52.6815 mL |
5 mM | 0.4215 mL | 2.1073 mL | 4.2145 mL | 10.5363 mL | |
10 mM | 0.2107 mL | 1.0536 mL | 2.1073 mL | 5.2681 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
MTI-31 1567915-38-1 PI3K/Akt/mTOR signaling mTOR mTOR kinase inhibitor tissue factor LXI 15029 mTORC2 mTOR inhibitor Inhibitor EGFR mutant cancer mTOR-TF axis Mammalian target of Rapamycin MTI31 apoptosis inhibit MTI 31 mTORC1 lipid metabolism LXI-15029 LXI15029 tumor microenvironment inhibitor