Apexbio Technology LLC Pacritinib (SB1518) 937272-79-2 10mM (in 1mL DMSO)

Supplier:  Apexbio Technology LLC B15895.1

Pacritinib (SB1518) is a small molecule inhibitor targeting Janus kinase 2 (JAK2) and Fms-like tyrosine kinase 3 (FLT3) with IC50 values of 23 nM for wild-type JAK2 19 nM for JAK2V617F and 22 nM for FLT3 It inhibits phosphorylation of downstream effectors such as STAT5 and STAT3 mediated by JAK2 in Ba/F3 cells as well as phosphorylation of FLT3 and STAT5 in MV4-11 cells Pacritinib demonstrates good microsomal stability selectivity limited inhibitory activity toward CYP3A4 favorable permeability in cell permeability assays and oral bioavailability In preclinical studies treatment with pacritinib in Ba/F3-JAK2V617F murine allograft and MV4-11 xenograft models reduces disease progression and enhances survival These properties make pacritinib suitable for research concerning hematologic malignancies involving dysregulated JAK2 or FLT3 signaling pathways

Catalog No. 50-000-63755