BI-4020

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

BI-4020 是第四代非共价、口服活性的 EGFR 酪氨酸激酶抑制剂。

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.

BI-4020 inhibits p-EGFR del19 T790M C797S with an IC50 of 0.6 nM.

BI-4020 leads to tumor regressions in the human PC-9 (EGFR del19 T790M C797S) triple mutant NSCLC xenograft model in mice.

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Angiogenesis

EGFR

Bacterial

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2664214-60-0

542.68

C30H38N8O2

>98% (HPLC)

In Vitro:?DMSO : 250 mg/mL (460.68 mM)

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

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(-20℃)

With Ice Pack

≥ 2 years