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ASP9853

Chemical Structure : ASP9853

CAS No.: 442198-67-6

ASP9853 (ASP 9853; ASP-9853; FR 260330 dehydrate)

Catalog No.: PC-60993Not For Human Use, Lab Use Only.

ASP9853 is 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.

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Biological Activity

ASP9853 is 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.
ASP9853 reduces NOx production in plasma from rats exposed to LPS (IC50=1.6 mg/kg), without effect on mean arterial blood pressure.
ASP9853 also shows greater tumor growth inhibition than docetaxel alone against non-small lung cancer xenografts in combination with docetaxe.

Physicochemical Properties

M.Wt 617.026
Formula C29H28ClF3N6O4
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(S,E)-3-(4-chlorophenyl)-N-(1-oxo-1-((2-oxo-2-(4-((6-(trifluoromethyl)pyrimidin-4-yl)oxy)piperidin-1-yl)ethyl)amino)-3-(pyridin-2-yl)propan-2-yl)acrylamide

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.

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