1. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  2. EGFR
  3. EGFR-IN-77

EGFR-IN-77 (Compound 4a) 是一种选择性的 EGFRT790M/L858R 抑制剂,针对 EGFRT790M/L858RIC50 为 0.101 μM,针对 EGFRL858RIC50 为 0.477 μM,针对野生型 EGFRIC50 为 1.771 μM。EGFR-IN-77 可在功能上抑制 EGFRT790M/L858REGFRL858R 及野生型 EGFR 的激酶活性。EGFR-IN-77 对 EGFRT790M/L858R 非小细胞肺癌细胞具有选择性的抗增殖作用。EGFR-IN-77 可用于 EGFRL858R/T790M 双突变非小细胞肺癌的研究。

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EGFR-IN-77

EGFR-IN-77 Chemical Structure

CAS No. : 2222930-49-4

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

EGFR-IN-77 (Compound 4a) is a selective EGFRT790M/L858R inhibitor, with an IC50 of 0.101 μM against EGFRT790M/L858R, 0.477 μM against EGFRL858R, and 1.771 μM against wild-type EGFR. EGFR-IN-77 functionally inhibits the kinase activities of EGFRT790M/L858R, EGFRL858R and wild-type EGFR. EGFR-IN-77 exerts selective antiproliferative effects on EGFRT790M/L858R non-small cell lung cancer cells. EGFR-IN-77 can be used for the research of EGFRL858R/T790M double-mutant non-small cell lung cancer[1].

IC50 & Target[1]

EGFRL858R/T790M

0.101 μM (IC50)

EGFRL858R

0.477 μM (IC50)

EGFRWT

1.771 μM (IC50)

体外研究
(In Vitro)

EGFR-IN-77 可抑制纯化的 TL 双突变 EGFR 激酶,其 IC50 为 0.101 μM;抑制 L858R 突变 EGFR 激酶的 IC50 为 0.477 μM;抑制野生型 (WT) EGFR 激酶的 IC50 为 1.771 μM,对 TL EGFR 的选择性是 WT EGFR 的 17.52 倍[1]
EGFR-IN-77 可抑制 H1975 (TL EGFR) 非小细胞肺癌细胞、PC9 (L858R EGFR) 细胞和 H292 (WT EGFR) 细胞的增殖,其对上述三种细胞的 IC50 分别为 0.184 μM、0.137 μM 和 8.321 μM,对 H1975 细胞的选择性较 H292 细胞高 45.27 倍[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

472.54

Formula

C26H28N6O3

CAS 号
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.

纯度 & 产品资料
参考文献
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
EGFR-IN-77
目录号:
HY-153605
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