An irreversible BMX inhibitor
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CHMFL-BMX-078

Item No. 36828

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
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
CAS Number
1808288-51-8
Molecular Formula
C33H35N7O6
Formula Weight
625.7
Purity
≥90%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Slightly soluble
SMILES
O=C(NC1=CC(NC2=NC=C(C(NC)=N2)C(NC3=CC(NC(C4=CC(OC)=C(C(OC)=C4)OC)=O)=CC=C3C)=O)=CC=C1C)C=C
InChi Code
InChI=1S/C33H35N7O6/c1-8-28(41)38-24-16-22(12-10-18(24)2)37-33-35-17-23(30(34-4)40-33)32(43)39-25-15-21(11-9-19(25)3)36-31(42)20-13-26(44-5)29(46-7)27(14-20)45-6/h8-17H,1H2,2-7H3,(H,36,42)(H,38,41)(H,39,43)(H2,34,35,37,40)
InChi Key
XURALSVDCFXBAX-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $98

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    10 mg

    $148

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    25 mg

    $269

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    50 mg

    $489

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    Product Description

    CHMFL-BMX-078 is an irreversible inhibitor of bone marrow tyrosine kinase on chromosome X (BMX; IC50 = 11 nM).1 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.2 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.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Liang, X., Lv, F., Wang, B., et al. Discovery of 2-((3-Acrylamido-4-methylphenyl)amino)-N-(2-methyl-5-(3,4,5-trimethoxybenzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-BMX-078) as a highly potent and selective type II irreversible bone marrow kinase in the X chromosome (BMX) kinase inhibitor. J. Med. Chem. 60(5), 1793-1816 (2017).

    2. Jiang, S., Jiang, T., Huang, H., et al. CHMFL-BMX-078, a BMX inhibitor, overcomes the resistance of melanoma to vemurafenib via inhibiting AKT pathway. Chem. Biol. Interact. 351, 109747 (2022).