| Identification | Back Directory | [Name]
INDEX NAME NOT YET ASSIGNED | [CAS]
2664214-60-0 | [Synonyms]
HER1,BI-4020,inhibit,BI4020,BI 4020,Epidermal growth factor receptor,ErbB-1,Inhibitor,EGFR | [Molecular Formula]
C30H38N8O2 | [MDL Number]
MFCD32693898 | [MOL File]
2664214-60-0.mol | [Molecular Weight]
542.69 |
| Chemical Properties | Back Directory | [Boiling point ]
736.6±70.0 °C(Predicted) | [density ]
1.33±0.1 g/cm3(Predicted) | [form ]
Solid | [pka]
7.60±0.10(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
BI-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 50]
EGFRdel19 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 |
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