1. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  2. EGFR
  3. EGFR-IN-139

EGFR-IN-139 (compound PD 18) 是一种 EGFR 抑制剂,IC50 分别为 12.88 (野生型),10.84 (L858R/T790M),42.68 (L858R/T790M/C797S) nM。EGFR-IN-139 对高度表达 EGFR 的 A549 和 H1975 癌细胞系显示出强烈的抗癌活性。EGFR-IN-139 对癌细胞具有很强的选择性。EGFR-IN-139 可用于非小细胞肺癌 (NSCLC) 的研究。

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EGFR-IN-139 Chemical Structure

EGFR-IN-139 Chemical Structure

CAS No. : 1574321-31-5

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

EGFR-IN-139 (compound PD 18) is an epidermal growth factor receptor (EGFR) inhibitor, with IC50s of 12.88 (wild type), 10.84 (L858R/T790M), 42.68 (L858R/T790M/C797S) nM, respectively. EGFR-IN-139 displays strong anticancer activity against A549 and H1975 cancer cell lines, which are highly expressed EGFR. EGFR-IN-139 has a strong selectivity to cancer cells. EGFR-IN-139 can be used for nonsmall cell lung cancer (NSCLC) research[1].

体外研究
(In Vitro)

EGFR-IN-139 (1μM, 2 h) 抑制野生型 EGFR 和 L858R/T790M EGFR,抑制率分别为 90-100% 和 65-75%[1]
EGFR-IN-139 (0-100 μM, 72 h) 抑制 A549,H1975,Vero 细胞,其 IC50 分别为 28.23,29.46,180.9 μM[1]

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

Cell Proliferation Assay

Cell Line: A549, H1975 cells
Concentration: 0-100 μM
Incubation Time: 72 h
Result: Inhibited A549, H1975, Vero cells with IC50s of 28.23 (similar to that of Erlotinib (HY-50896)), 29.46, 180.9 μM,.
Was relatively safe for normal cells, as its IC50 value in Vero cells was higher compared to those in A549 (SI(IC50 of A549 and H1975) versus IC50 of Vero) of 6.40) and H1975 (SI of 6.14).
分子量

476.95

Formula

C27H25ClN2O4

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-139
目录号:
HY-170438
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