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mTOR inhibitor 10

Names

[ CAS No. ]:
1222999-54-3

[ Name ]:
mTOR inhibitor 10

[Synonym ]:
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

Biological Activity

[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

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Boiling Point ]:
862.8±65.0 °C at 760 mmHg

[ Molecular Formula ]:
C41H32F3N5O2

[ Molecular Weight ]:
683.720

[ Flash Point ]:
475.6±34.3 °C

[ Exact Mass ]:
683.250793

[ LogP ]:
6.10

[ Vapour Pressure ]:
0.0±3.3 mmHg at 25°C

[ Index of Refraction ]:
1.723


Related Compounds