CHMFL-BMX-078

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

CHMFL-BMX-078 是一种高选择性、有效的 II 型不可逆 BMX 激酶抑制剂，IC50 为 11 nM。

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.

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.

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.

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

Tyrosine Kinase

BMX Kinase

Bmx

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1808288-51-8

625.686

C33H35N7O6

>98% (HPLC)

DMSO: Soluble （ < 1 mg/ml refers to the product slightly soluble or insoluble )

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

2-((3-Acrylamido-4-methylphenyl)amino)-N-(2-methyl-5-(3,4,5-trimethoxybenzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide

(-20℃)

With Ice Pack

≥ 2 years