RGNCY-0014 (JAK2 Inhibitor)

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NMS-P953 is a novel, potent and orally bioavailable JAK2 inhibitor with selectivity over other JAK family members (JAK3 5-fold, TYK2 24-fold and JAK1 110-fold). This compound displayed significant tumor growth inhibition in a SET-2 xenograft tumor model with a favorable pharmacokinetic and safety profile. JAK2 IC50 = 0.008 uM. 

SMILES: ClC1=CC=C(C(F)(F)F)C=C1C2=C(C(N)=O)C=C(C3=NC(N)=NC=C3)N2

Systematic Name: 5-(2-aminopyrimidin-4-yl)-2-(2-chloro-5-(trifluoromethyl)phenyl)-1H-pyrrole-3-carboxamide

Molecular Weight: 381.74

Formula: C29H33NO4

PMID: 25009002

Reference: Brasca, Maria Gabriella, et al. "Pyrrole-3-carboxamides as potent and selective JAK2 inhibitors." Bioorganic & Medicinal Chemistry 22.17 (2014): 4998-5012.

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Tags: Cancer, JAK2, RGNCY-0014, Tumor, SET-2