CHMFL-BMX-078 - 10mM in DMSO , CAS No.1808288-51-8

CAS: 1808288-51-8 Cat. No.: C656605 Fórmula: C₃₃H₃₅N₇O₆ Peso molecular: 625.67

GRADE & PURITY 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Visão geral

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.

IC50& Target:IC50: 11 nM (BMX)

Specifications

Especificações e pureza

10mM in DMSO

Mecanismos bioquímicos e fisiológicos

CHMFL-BMX-078 is a highly potent and selective type II irreversible BMX kinase inhibitor with an IC 50 of 11 nM.

Condições de armazenamento de armazenamento

Store at -80°C

Enviado em

Dry ice packs + Cold packs

Este produto requer transporte de cadeia fria. Serviços terrestres e outros serviços econômicos não estão disponíveis.

Tipo de ação

INHIBITOR

Nomes e identificadores

• Peso molecular: 625.67

Perguntas frequentes

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 1808288-51-8, the molecular formula is C33H35N7O6, and the molecular weight is 625.67 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.