1222999-54-3

1222999-54-3 structure

Name: mTOR inhibitor 10
Chemical Name: N-(1-Methyl-4-piperidinyl)-4'-[2-oxo-9-(3-quinolinyl)benzo[h][1,6]naphthyridin-1(2H)-yl]-2'-(trifluoromethyl)-4-biphenylcarboxamide
CAS Number: 1222999-54-3
Molecular Formula: C₄₁H₃₂F₃N₅O₂
Molecular Weight: 683.720
Create Date: 2020-01-11 18:31:50
Modify Date: 2024-01-19 10:57:03
A novel potent, selective mTOR inhibitor with biochemical IC50 of 21.7 nM for mTORC1, exhibits cellular potency against mTOR with IC50 of 5 nM; displays >50-fold selectivity over PIKKs (hVSP34, PI3Ks, PI4K, etc.); exhibits significant inhibitory activity against the downstream targets of mTOR, S6K, and Akt, and blocks 80-90% phosphorylation of S6K (T389) and pAkt (S473) in liver and lung tissues, along with significantly improved mouse liver microsome stability and a longer in vivo half-life.

Name	N-(1-Methyl-4-piperidinyl)-4'-[2-oxo-9-(3-quinolinyl)benzo[h][1,6]naphthyridin-1(2H)-yl]-2'-(trifluoromethyl)-4-biphenylcarboxamide
Synonyms	N-(1-Methyl-4-piperidinyl)-4'-[2-oxo-9-(3-quinolinyl)benzo[h][1,6]naphthyridin-1(2H)-yl]-2'-(trifluoromethyl)-4-biphenylcarboxamide [1,1'-Biphenyl]-4-carboxamide, N-(1-methyl-4-piperidinyl)-4'-[2-oxo-9-(3-quinolinyl)benzo[h][1,6]naphthyridin-1(2H)-yl]-2'-(trifluoromethyl)- MFCD27992058

Description	A novel potent, selective mTOR inhibitor with biochemical IC50 of 21.7 nM for mTORC1, exhibits cellular potency against mTOR with IC50 of 5 nM; displays >50-fold selectivity over PIKKs (hVSP34, PI3Ks, PI4K, etc.); exhibits significant inhibitory activity against the downstream targets of mTOR, S6K, and Akt, and blocks 80-90% phosphorylation of S6K (T389) and pAkt (S473) in liver and lung tissues, along with significantly improved mouse liver microsome stability and a longer in vivo half-life.
References	References 1. Liu Q, et al. Bioorg Med Chem Lett. 2011 Jul 1;21(13):4036-40. View Related Products by Target mTOR