1H-4,8-Metheno-17H-pyrazolo[3′,4′:2,3][1,5,10,12]oxatriazacycloheptadecino[12,11-a]benzimidazol-9(11H)-one, 18,19,20,21-tetrahydro-1,6,18-trimethyl-14-[(4-methyl-1-piperazinyl)methyl]-, (10E,18R)-

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1H-4,8-Metheno-17H-pyrazolo[3′,4′:2,3][1,5,10,12]oxatriazacycloheptadecino[12,11-a]benzimidazol-9(11H)-one, 18,19,20,21-tetrahydro-1,6,18-trimethyl-14-[(4-methyl-1-piperazinyl)methyl]-, (10E,18R)- Suppliers list
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1H-4,8-Metheno-17H-pyrazolo[3′,4′:2,3][1,5,10,12]oxatriazacycloheptadecino[12,11-a]benzimidazol-9(11H)-one, 18,19,20,21-tetrahydro-1,6,18-trimethyl-14-[(4-methyl-1-piperazinyl)methyl]-, (10E,18R)- manufacturers

  • BI-4020
  • BI-4020 pictures
  • $173.00
  • 2026-07-27
  • CAS:2664214-60-0
  • Purity: 99.74%
  • Supply Ability: 10g
  • BI-4020
  • BI-4020 pictures
  • $173.00
  • 2026-07-27
  • CAS:2664214-60-0
  • Purity: 99.74%
  • Supply Ability: 10g
1H-4,8-Metheno-17H-pyrazolo[3′,4′:2,3][1,5,10,12]oxatriazacycloheptadecino[12,11-a]benzimidazol-9(11H)-one, 18,19,20,21-tetrahydro-1,6,18-trimethyl-14-[(4-methyl-1-piperazinyl)methyl]-, (10E,18R)- Basic information
Product Name:1H-4,8-Metheno-17H-pyrazolo[3′,4′:2,3][1,5,10,12]oxatriazacycloheptadecino[12,11-a]benzimidazol-9(11H)-one, 18,19,20,21-tetrahydro-1,6,18-trimethyl-14-[(4-methyl-1-piperazinyl)methyl]-, (10E,18R)-
Synonyms:HER1,BI-4020,inhibit,BI4020,BI 4020,Epidermal growth factor receptor,ErbB-1,Inhibitor,EGFR;BI-4020, 10 mM in DMSO;1H-4,8-Metheno-17H-pyrazolo[3′,4′:2,3][1,5,10,12]oxatriazacycloheptadecino[12,11-a]benzimidazol-9(11H)-one, 18,19,20,21-tetrahydro-1,6,18-trimethyl-14-[(4-methyl-1-piperazinyl)methyl]-, (10E,18R)-
CAS:2664214-60-0
MF:C30H38N8O2
MW:542.68
EINECS:
Product Categories:
Mol File:2664214-60-0.mol
1H-4,8-Metheno-17H-pyrazolo[3′,4′:2,3][1,5,10,12]oxatriazacycloheptadecino[12,11-a]benzimidazol-9(11H)-one, 18,19,20,21-tetrahydro-1,6,18-trimethyl-14-[(4-methyl-1-piperazinyl)methyl]-, (10E,18R)- Structure
1H-4,8-Metheno-17H-pyrazolo[3′,4′:2,3][1,5,10,12]oxatriazacycloheptadecino[12,11-a]benzimidazol-9(11H)-one, 18,19,20,21-tetrahydro-1,6,18-trimethyl-14-[(4-methyl-1-piperazinyl)methyl]-, (10E,18R)- Chemical Properties
Boiling point 736.6±70.0 °C(Predicted)
density 1.33±0.1 g/cm3(Predicted)
pka7.60±0.10(Predicted)
form Solid
color Light yellow to yellow
Safety Information
MSDS Information
1H-4,8-Metheno-17H-pyrazolo[3′,4′:2,3][1,5,10,12]oxatriazacycloheptadecino[12,11-a]benzimidazol-9(11H)-one, 18,19,20,21-tetrahydro-1,6,18-trimethyl-14-[(4-methyl-1-piperazinyl)methyl]-, (10E,18R)- Usage And Synthesis
UsesBI-4020 is a fourth-generation, orally active, and non-covalent EGFR tyrosine kinase inhibitor. BI-4020 inhibits not only the triple mutant EGFR del19 T790M C797S variant (IC50=0.2 nM in BaF3 cell lines) but also the double mutant EGFR del19 T790M and primary mutant EGFR del19 (IC50=1 nM). BI-4020 also shows activity against EGFR wt (IC50=190 nM). BI-4020 shows high kinome selectivity and good DMPK properties[1].
in vivo

BI-4020 leads to tumor regressions in the human PC-9 (EGFR del19 T790M C797S) triple mutant NSCLC xenograft model in mice[1].

IC 50EGFRdel19 T790M C797S: 0.2 nM (IC50); EGFRdel19: 1 nM (IC50); EGFRWT: 190 nM (IC50); EGFRdel19 T790M
References[1] Engelhardt H,et al. Start selective and rigidify: The discovery path towards a next generation of EGFR tyrosine kinase inhibitors. J Med Chem. 2019 Nov 5. DOI:10.1021/acs.jmedchem.9b01169
1H-4,8-Metheno-17H-pyrazolo[3′,4′:2,3][1,5,10,12]oxatriazacycloheptadecino[12,11-a]benzimidazol-9(11H)-one, 18,19,20,21-tetrahydro-1,6,18-trimethyl-14-[(4-methyl-1-piperazinyl)methyl]-, (10E,18R)- Preparation Products And Raw materials
Tag:1H-4,8-Metheno-17H-pyrazolo[3′,4′:2,3][1,5,10,12]oxatriazacycloheptadecino[12,11-a]benzimidazol-9(11H)-one, 18,19,20,21-tetrahydro-1,6,18-trimethyl-14-[(4-methyl-1-piperazinyl)methyl]-, (10E,18R)-(2664214-60-0) Related Product Information
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