Mutated EGFR-IN-2

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Mutated EGFR-IN-2 

Mutated EGFR-IN-2 (compound 91) 突变选择性的 EGFR 抑制剂,有效抑制单突变体 EGFR (T790M) 和双突变体 EGFR (包括 L858R/T790M (IC50=<1nM) 和 ex19del/T790M),并且可以抑制单一功能获得性突变 EGFR (包括 L858R 和 ex19del) 的活性。Mutated EGFR-IN-2 具有抗肿瘤活性。

Mutated EGFR-IN-2

Mutated EGFR-IN-2 Chemical Structure

CAS No. : 2050906-97-1

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生物活性

Mutated EGFR-IN-2 (compound 91) is a mutant-selective EGFR inhibitor extracted from patent WO2017036263A1, which potently inhibits single-mutant EGFR (T790M) and double-mutant EGFR (including L858R/T790M (IC50=<1nM) and ex19del/T790M), and can suppress activity of single gain-of-function mutant EGFR (including L858R and ex19del) as well. Mutated EGFR-IN-2 shows anti-tumor antivity[1].

IC50 & Target[1]

EGFRT790M

 

EGFRL858R

 

EGFRex19del

 

EGFR (L858R/T790M)

<1 nM (IC50)

EGFR (ex19del/T790M)

 

分子量

562.64

Formula

C29H35FN8O3

CAS 号

2050906-97-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. 2, 4-di-(nitrogen containing group) substituted pyrimidine compound and preparation method and use thereof.

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