BI-4020
BI-4020 is a fourth-generation, non-covalent, and orally active inhibitor of EGFR tyrosine kinase. (In Vitro) :BI-4020 inhibits p-EGFR del19 T790M C797S (IC50: 0.6 nM) . 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. (In Vivo) :In the human PC-9 (EGFR del19/T790M/C797S) triple mutant NSCLC xenograft model in mice, BI-4020 leads to tumor regressions.
Product Specifications
CAS Number
2664214-60-0
Purity
>98% (HPLC)
Solubility
In Vitro: DMSO : 250 mg/mL (460.68 mM)
Smiles
O=C (C1=CC (C) =NC (C2=C (OCCC[C@@H] (C) C3) N (C) N=C2) =C1) /N=C (N4) /N3C5=C4C=CC (CN6CCN (C) CC6) =C5
Molecular Formula
C30H38N8O2
Molecular Weight
542.68
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
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