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首页-小分子抑制剂&激动剂-PI3K/Akt/mTOR Pathway-mTOR-MTI-31
MTI-31

Chemical Structure : MTI-31

CAS No.: 1567915-38-1

MTI-31 (LXI-15029;mTOR inhibitor-31)

货号: PC-36112Not For Human Use, Lab Use Only.

MTI-31 (LXI-15029, mTOR inhibitor-31) is a novel potent, selective mTORC1/mTORC2 inhibitor with Kd of 0.2 nM (mTOR), displays >5,000-fold selectivity over PIK3CA, PIK3CB and PIK3G.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

MTI-31 (LXI-15029, mTOR inhibitor-31) is a novel potent, selective mTORC1/mTORC2 inhibitor with Kd of 0.2 nM (mTOR), displays >5,000-fold selectivity over PIK3CA, PIK3CB and PIK3G.
MTI-31 showed an IC50 value 39 nM in LANCE® assay of mTOR substrate phosphorylation.
MTI-31 dose-dependently inhibits of both the mTORC1 substrates P-S6K1(T389), P-S6(S235/6), P-4EBP1(T70) and mTORC2 substrate P-AKT(S473) tumor cell lines harboring mTOR pathway dysregulation with IC50 of <0.12 uM.
MTI-31 potently inhibited cell proliferation (IC50 <1 mmol/L) and in vivo tumor growth in multiple NSCLC models of EGFR/T790M, EML4-ALK, c-Met or KRAS (MED <10 mg/kg), also suppressed programmed death ligand 1 (PD-L1) in EGFR- and ALK-driven NSCLC, mediated in part by mTORC2/AKT/GSK3β-dependent proteasomal degradation.

物理化学性质&存储条件

分子量 474.565
分子式 C26H30N6O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

3-(4-(3-oxa-8-azabicyclo[3.2.1]octan-8-yl)-2-((S)-3-methylmorpholino)pyrido[2,3-d]pyrimidin-7-yl)-N-methylbenzamide

参考文献

1. Qian J, et al. Oncotarget. 2016 Oct 11;7(41):67071-67086.

2. Zhang Q, et al. Clin Cancer Res. 2019 Feb 22. pii: clincanres.2548.2018.

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