CHMFL-BMX-078

SKU: orb1225886

Description

CHMFL-BMX-078 is a highly selective, potent, type II irreversible BMX kinase inhibitor with IC50 of 11 nM; displays a high selectivity profile (S score(1) = 0.01) against the 468 kinases/mutants in the KINOMEscan evaluation and achieved at least 40-fold selectivity over BTK kinase; CHMFL-BMX-078 is a useful pharmacological tool to elucidate the detailed mechanism of BMX mediated signaling pathways.

Key Properties

• CAS Number: 1808288-51-8
• MW: 625.686
• Purity: >98% (HPLC)
• Formula: C₃₃H₃₅N₇O₆
• SMILES: O=C(C1=CN=C(NC2=CC=C(C)C(NC(C=C)=O)=C2)N=C1NC)NC3=CC(NC(C4=CC(OC)=C(OC)C(OC)=C4)=O)=CC=C3C
• Target: BMX Kinase
• Solubility: DMSO: Soluble （ < 1 mg/ml refers to the product slightly soluble or insoluble )

Bioactivity

• In Vivo:
  CHMFL-BMX-078 exhibits a short half-life (T1/2 = 0.80 h) in iv injection. CHMFL-BMX-078 also displays an acceptable Cmax (13565.23 ng/mL) and AUC0-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.
• 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 IC50 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 (IC50 = 437 nM). For inactive state of BMX kinase, CHMFL-BMX-078 displays a binding Kd of 81 nM, while for the active state of BMX kinase, it exhibits a binding Kd of 10200 nM. CHMFL-BMX-078 exhibits antiproliferative effects against BaF3-TEL-BMX cells (GI50 = 0.016 μM) and selectivity over parental BaF3 cells. CHMFL-BMX-078 is about 80-fold more potent against BMX wt (EC50 = 5.8 nM) than C496S mutant (EC50 = 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CHMFL-BMX-078 | CHMFL-BMX 078 | CHMFL BMX 078 | CHMFLBMX078

Quick Database Links

Gene Symbol

BMX Kinase