CHMFL-BMX-078 is a highly potent and selective type II irreversible BMX kinase inhibitor with an IC 50 of 11 nM. In Vitro Bone marrow kinase in the X chromosome (BMX, also called ETK) is a nonreceptor tyrosine kinase involved in tumorigenicity, cell motility, adhesion, angiogenesis, proliferation, and differentiation. CHMFL-BMX-078 exhibits an IC 50 of 11 nM by formation of a covalent bond with cysteine 496 residue in the DFG-out inactive conformation of BMX. It displays a high selectivity profile against the 468 kinases/mutants in the KINOMEscan evaluation and achieves at least 40-fold selectivity over BTK kinase (IC 50 =437 nM). For inactive state of BMX kinase, CHMFL-BMX-078 displays a binding K d of 81 nM, while for the active state of BMX kinase, it exhibits a binding K d of 10200 nM. CHMFL-BMX-078 exhibits antiproliferative effects against BaF3-TEL-BMX cells (GI 50 =0.016 μM) and selectivity over parental BaF3 cells. CHMFL-BMX-078 is about 80-fold more potent against BMX wt (EC 50 =5.8 nM) than C496S mutant (EC 50 =459 nM) for the inhibition of BMX total tyrosine phosphorylation. CHMFL-BMX-078 would serve as a useful pharmacological tool to elucidate the detailed mechanism of BMX mediated signaling pathways. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo CHMFL-BMX-078 exhibits a short half-life (T 1/2 =0.80 h) in iv injection. CHMFL-BMX-078 also displays an acceptable C max (13565.23 ng/mL) and AUC 0-t (1386.41 ng/mL h) in iv injection. However, it is not absorbed by oral administration, indicating that this compound could be administrated through iv or ip injection when used as a research tool . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:IC50: 11 nM (BMX)
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CHMFL-BMX-078
CAS number：1808288-51-8 molecular formula：C33H35N7O6
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| Chinese alias | - | ||
| English alias | - | ||
| CAS number | 1808288-51-8 | molecular formula | C33H35N7O6 |
| molecular weight | 625.67 g/mol | Exact mass | ≥98% |
| PSA | - | logp | - |
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