1. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  2. EGFR
  3. EGFR-IN-50

EGFR-IN-50 (Compound 9h) 是一种针对 L858R 抗性突变的强效 EGFR 抑制剂 (TEL-EGFR-L858R-BaF3: GI50=8 nM, TEL-EGFR-T790M-L858R-BaF3: GI50=6.03 μM) 。EGFR-IN-50 表现出对癌细胞的抗增殖活性。

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EGFR-IN-50 Chemical Structure

EGFR-IN-50 Chemical Structure

CAS No. : 2044508-48-5

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

EGFR-IN-50 (Compound 9h) is a potent EGFR inhibitor against L858R resistance mutation (TEL-EGFR-L858R-BaF3: GI50=8 nM, TEL-EGFR-T790M-L858R-BaF3: GI50=6.03 μM). EGFR-IN-50 shows anti-proliferative activity to cancer cells[1].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HUVEC IC50
> 10 μM
Compound: 9h
Cytotoxicity against HUVEC assessed as reduction in cell viability measured after 72 hrs by Celltiter-Glo luminescent cell viability assay
Cytotoxicity against HUVEC assessed as reduction in cell viability measured after 72 hrs by Celltiter-Glo luminescent cell viability assay
[PMID: 32619886]
体外研究
(In Vitro)

EGFR-IN-50 (0-10 μM; 72 h) selectively inhibits NSCLC cell line H3255 (expressing EGFR-L858R) compared to other tumor cells[1].
EGFR-IN-50 (1-10 μM; 72 h) induces cell cycle arrest in G0-G1 phase[1].
EGFR-IN-50 (0.039-10 μM; 4 h) inhibits the phosphorylation of EGFR in H3255 cells[1].

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

Cell Proliferation Assay[1]

Cell Line: A549, H3255, HepG2, MCF-7, HT-29 and A431 cells
Concentration: 0-10 μM
Incubation Time: 72 hours
Result: Showed GI50 values of >10, and 0.7873 μM for A549 and H3255 cells, respectively.
Showed IC50 values of >10, 7.309, >10 and 6.703 μM for HepG2, MCF-7, HT-29 and A431 cells, respectively.

Cell Cycle Analysis[1]

Cell Line: H3255 cells
Concentration: 1, 5, and 10 μM
Incubation Time: 72 hours
Result: Increased the percentage of H3255 cells in G0-G1 phase from 60.32% to 88.61%.

Western Blot Analysis[1]

Cell Line: H3255 cells
Concentration: 0.039, 0.15, 0.62, 2.5, and 10 μM
Incubation Time: 4 hours
Result: Inhibited the phosphorylation of EGFR in H3255 cells in a dose-dependent manner.
分子量

564.51

Formula

C24H26BrN3O4S2

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-50
目录号:
HY-146210
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