Formulation: A solid
Formal Name: 4-(methylamino)-2-[[4-methyl-3-[(1-oxo-2-propen-1-yl)amino]phenyl]amino]-N-[2-methyl-5-[(3,4,5-trimethoxybenzoyl)amino]phenyl]-5-pyrimidinecarboxamide
Purity: ≥90%
Formula Markup: C33H35N7O6
Formula Weight: 625,7
Shelf life (days): 1460
CAS Number: 1808288-51-8
Notes: CHMFL-BMX-078 is an irreversible inhibitor of bone marrow tyrosine kinase on chromosome X (BMX; IC50 = 11 nM).{65431} It selectively inhibits the growth of Ba/F3 cells expressing BMX over Ba/F3 cells expressing Abl, c-Kit, PDGFRα, or PDGFRβ (GI50s = 0.016, 2.56, 2.01, 0.67, and 0.91 µM, respectively), as well as Ba/F3 cells expressing FLT3, EGFR, JAK3, or Blk (GI50s = >10 µM for all). CHMFL-BMX-078 inhibits the growth of 22Rv1, DU145, and PC3 prostate, Hb-c, J82, and T24 bladder, and ACHN renal cancer cells (GI50s = 3.45-7.89, 5.78-8.98, and 4.93 µM, respectively). It restores cytotoxicity induced by vemurafenib (PLX4032; Item No. 10618) in vemurafenib-resistant A375 melanoma cells.{65432} CHMFL-BMX-078 (15 mg/kg) reduces tumor weight and enhances vemurafenib-induced reduction of tumor weight in a vemurafenib-resistant A375 mouse xenograft model.
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