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Background Information:
Decernotinib (VX-509; VRT-831509, Adelatinib) is an orally bioavailable Janus kinase 3 (JAK3) inhibitor, potently and selectively inhibiting the enzyme with an in vitro Ki of 2.5 nM, and IC50 of 50-170 nM in cellular assays dependent on JAK3 activity. Highly selective, displaying no activity (with limited or no measureable potency) towards other JAK and non-JAK enzymes. Showed in vivo activity in two animal models of aberrant immune function, and demonstrated dose-dependent reduction in ankle swelling and paw weight and improved paw histopathology scores in the rat collagen-induced arthritis model (ref.1).
Reference:
1. S. Mahajan, et al, VX-509 is a potent and selective Janus kinase 3 (JAK3) inhibitor that attenuates inflammation in animal models of autoimmune disease. J .Pharmacol Exp Ther. 2015 May;353(2):405-14. doi: 10.1124/jpet.114.221176. Epub 2015 Mar 1.
APIM050140: DECERNOTINIB (VX-509)
CAS No.: 944842-54-0.
Molecular Formula: C18H19F3N6O.
Molecular Weight: 392.4.
Purity: 100% optical purity (Chiral HPLC), >99.5% purity (HPLC at 214 and 254 nm).
QC: HPLC-MS, 1HNMR, Chiral HPLC, and Quantitative Elemental Analysis.
Solubility: Soluble in DMSO.
Storage: Store at 0-4°C (short term), -20°C (long term), desiccated.
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