BI-4020

立即咨询

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。

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 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
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 tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation 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.