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ChemicalBook > Product Catalogue >Biochemical Engineering >Inhibitors >protein tyrosine kinase >WZ8040

WZ8040

WZ8040 Structure
  • ₹0
  • Product name: WZ8040
  • CAS: 1214265-57-2
  • MF: C24H25ClN6OS
  • MW: 481.01
  • EINECS:-0
  • MDL Number:MFCD18074511
  • Synonyms:WZ8040;N-[3-[[5-Chloro-2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]thio]phenyl]-2-propenamide;N-(3-(5-chloro-2-(4-(4-methylpiperazin-1-yl)phenylamino)pyrimidin-4-ylthio)phenyl)acrylamide;N-[3-[[5-Chloro-2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]thio]phenyl]-2-propenamide WZ8040;N-(3-((5-Chloro-2-((4-(4-methylpiperazin-1-yl)phenyl)amino)pyrimidin-4-yl)thio)phenyl)acrylami;CS-471;WZ-8040;WZ 8040;2-Propenamide, N-[3-[[5-chloro-2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]thio]phenyl]-
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Properties

Density :1.37
storage temp. :Store at -20°C
solubility :≥24.05 mg/mL in DMSO; insoluble in H2O; ≥2.61 mg/mL in EtOH with gentle warming and ultrasonic
form :solid
pka :12.94±0.70(Predicted)
color :Light yellow to green yellow

Safety Information

Symbol(GHS):
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Code Hazard statements Hazard class Category Signal word Pictogram P-Codes
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Description

WZ8040 is an inhibitor of mutant EGF receptors (EGFRs) with IC50 values ranging from 2 to 306 nM in Ba/F3 cells. It is selective for EGFR mutants, including the EGFRDel E746_A750 and EGFRL858R mutations conferring gefitinib sensitivity and the EGFRDel E746_A750/T790M mutation conferring gefitinib resistance (IC50s = 2, 6, and 6 nM in Ba/F3 cells), over wild-type EGFR (IC50 = 1,820 nM in HN11 cells) but also inhibits ERBB2Ins G776V,C and wild-type ERBB2 (IC50s = 20 and 32 nM, respectively, in Ba/F3 cells). WZ8040 inhibits proliferation of PC-9 cells harboring the EGFRDel E746_A750 mutation and gefitinib-resistant PC-9 GR cells harboring the EGFRT790M resistant allele (EC50s = 6 and 8 nM, respectively).

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