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CHMFL-BMX-078

This product is for research use only, not for human use. We do not sell to patients.

CHMFL-BMX-078
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Cat #: V2990 CAS #: 1808288-51-8 Purity ≥ 98%

Description: CHMFL-BMX-078 is a highly potent and selective type II irreversible/covalent kinase inhibitor of BMX (bone marrow kinase on chromosome X) kinase with an IC50 of 11 nM.

References: Liang X, 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

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Molecular Weight (MW)625.67
Molecular FormulaC33H35N7O6
CAS No.1808288-51-8
Storage-20℃ for 3 years in powder formr
-80℃ for 2 years in solvent
Solubility In VitroDMSO: ≥ 30 mg/mLr
Water: <1 mg/mLr
Ethanol: <1 mg/mL
SMILES CodeO=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
SynonymsCHMFL BMX 078; CHMFL-BMX-078; CHMFL-BMX 078; CHMFLBMX078
ProtocolIn VitroBone 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.
In VivoCHMFL-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.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM1.5983 mL7.9914 mL15.9829 mL31.9657 mL
5mM0.3197 mL1.5983 mL3.1966 mL6.3931 mL
10mM0.1598 mL0.7991 mL1.5983 mL3.1966 mL
20mM0.0799 mL0.3996 mL0.7991 mL1.5983 mL
Quality Control Documentation
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Step Two: Enter the in vivo formulation
%DMSO + % + %Tween 80 + %ddH2O
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Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation: Take µL DMSO master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH2O,mix and clarify.
Note:
  • (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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