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BI-4020
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
BI-4020图片
包装与价格:
包装价格(元)
1mg电议
5mg电议

产品介绍
BI-4020 是第四代口服活性非共价 EGFR 酪氨酸激酶抑制剂。 BI-4020 不仅抑制三突变 EGFR del19 T790M C797S 变体(在 BaF3 细胞系中 IC50=0.2 nM),而且抑制双突变 EGFR del19 T790M 和原发突变 EGFR del19 (IC50=1 nM)。 BI-4020 还显示出针对 EGFR wt (IC50=190 nM) 的活性。 BI-4020 显示出高激酶组选择性和良好的 DMPK 特性。
Canonical SMILESO=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
分子式C30H38N8O2
分子量542.68
溶解度DMSO: 250 mg/mL (460.68 mM)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.