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MTI-31
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
MTI-31图片
CAS NO:1567915-38-1
包装与价格:
包装价格(元)
1 mg电议
2 mg电议
5 mg电议
10 mg电议
25 mg电议
100 mg电议

产品名称
LXI-15029
产品介绍
MTI-31 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。

产品描述

MTI-31 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].

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].

Cas No.

1567915-38-1

分子式

C26H30N6O3

分子量

474.55

别名

MTI-31;LXI-15029

储存和溶解度

DMSO:8.33 mg/mL (17.55 mM),Need ultrasonic and warming and heat to 60°C
Powder: -20°C for 3 years
In solvent: -80°C for 2 years