442198-67-6

442198-67-6 structure

Name: ASP 9853
Chemical Name: FK-330
CAS Number: 442198-67-6
Molecular Formula: C₂₉H₂₈ClF₃N₆O₄
Molecular Weight: 617.019
Create Date: 2020-01-11 11:44:37
Modify Date: 2024-01-17 19:36:40
A potent, orally active iNOS inhibitor (IC50=10 nM, NO release DLD-1 cells) that prevents dimerization of iNOS, but has no effect on the expression or enzyme activity of iNOS; reduces NOx production in plasma from rats exposed to LPS (IC50=1.6 mg/kg), without effect on mean arterial blood pressure; also shows greater tumor growth inhibition than docetaxel alone against non-small lung cancer xenografts in combination with docetaxe. Blood Cancer Phase 1 Discontinued

Name	FK-330
Synonyms	FK-330 N2-[(2E)-3-(4-Chlorophenyl)-2-propenoyl]-N-[2-oxo-2-(4-{[6-(trifluoromethyl)-4-pyrimidinyl]oxy}-1-piperidinyl)ethyl]-3-(2-pyridinyl)-L-alaninamide K47C68D94B 2-Pyridinepropanamide, α-[[(2E)-3-(4-chlorophenyl)-1-oxo-2-propen-1-yl]amino]-N-[2-oxo-2-[4-[[6-(trifluoromethyl)-4-pyrimidinyl]oxy]-1-piperidinyl]ethyl]-, (αS)-

Description	A potent, orally active iNOS inhibitor (IC50=10 nM, NO release DLD-1 cells) that prevents dimerization of iNOS, but has no effect on the expression or enzyme activity of iNOS; reduces NOx production in plasma from rats exposed to LPS (IC50=1.6 mg/kg), without effect on mean arterial blood pressure; also shows greater tumor growth inhibition than docetaxel alone against non-small lung cancer xenografts in combination with docetaxe. Blood Cancer Phase 1 Discontinued
References	References 1. Luke JJ, et al. Cancer Chemother Pharmacol. 2016 Mar;77(3):549-58. 2. Chida N, et al. Eur J Pharmacol. 2005 Feb 10;509(1):71-6. View Related Products by Target Nitric Oxide Synthase (NOS) Blood Cancer