BI-4020 |
| カタログ番号GC38402 |
BI-4020 は、第 4 世代の経口活性型非共有 EGFR チロシンキナーゼ阻害剤です。 BI-4020 は、三重変異体 EGFR del19 T790M C797S バリアント (BaF3 細胞株で IC50=0.2 nM) だけでなく、二重変異体 EGFR del19 T790M および一次変異体 EGFR del19 (IC50=1 nM) も阻害します。 BI-4020 は、EGFR wt に対する活性も示します (IC50 = 190 nM)。 BI-4020 は、高いキノーム選択性と優れた DMPK 特性を示します。
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Cas No.: 2664214-60-0
Sample solution is provided at 25 µL, 10mM.
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BI-4020 is a fourth-generation, orally active, and non-covalent EGFR tyrosine kinase inhibitor, which 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) whilst sparing activity against EGFR wt (IC50=190 nM). BI-4020 shows high kinome selectivity and good DMPK properties[1].
BI-4020 inhibits p-EGFR del19 T790M C797S with an IC50 of 0.6 nM[1].
BI-4020 leads to tumor regressions in the human PC-9 (EGFR del19 T790M C797S) triple mutant NSCLC xenograft model in mice[1].
[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.
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