Mutated EGFR-IN-2

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Mutated EGFR-IN-2

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CAS NO:

2050906-97-1

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。

生物活性

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

IC₅₀& Target^[1]

EGFR^T790M

EGFR^L858R

EGFR^ex19del

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.