BMS-911543

Description	BMS-911543 is a pyrrolopyridine small-molecule inhibitor. Dissociation constants of BMS-911543 for JAK1, JAK2 and JAK3 extended these findings and displays a broader selectivity for JAK2 with Ki values of 1114, 0.48 and 357?nm, respectively. Outside the JAK family, the highest inhibitory activity is observed for the Src family member, Lyn (IC50=300?nm), and the c-FMS receptor tyrosine kinase (IC50=450?nm), which are both significantly less sensitive than JAK2 (>250-fold). In JAK2V617F-dependent cells such as SET2 or Ba/F3 engineered to express JAK2V617F, BMS-911543 treatment resulted in a dose-dependent anti-proliferative effect with IC50 values of 60 and 70?nm, respectively. BMS-911543 suppresses the growth of MPN patient-derived cells. In the presence of EPO, BFU-E IC50s for BMS-911543 in MPN-patient cells rangs from <0.150 to ~0.9?μm, indicating an increased sensitivity to JAK2 inhibition compared with normal healthy volunteers. BMS-911543 inhibits TPO-stimulated JAK2WT-pSTAT5 activ
Pathways	Angiogenesis/Protein Tyrosine Kinase Jak/Stat Pathway Wnt/Stem Cell Epigenetics
Targets	JAK

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