1. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  2. EGFR
  3. EGFR/HER2-IN-8

EGFR/HER2-IN-8 (compound 34) 是 EGFR/HER2DHFR 的抑制剂。EGFR/HER2-IN-8 抑制 EGFR 激酶,HER2 激酶和 DHFR,其 IC50 值分别为 0.45,0.244 和 5.669 μM。EGFR/HER2-IN-8 对多种癌细胞具有抗癌活性,具有较高的安全性和选择性指数。EGFR/HER2-IN-8 可用于癌症的研究。

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EGFR/HER2-IN-8 Chemical Structure

EGFR/HER2-IN-8 Chemical Structure

CAS No. : 2820126-32-5

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

EGFR/HER2-IN-8 (compound 34) is a EGFR/HER2 and DHFR inhibitor. EGFR/HER2-IN-8 inhibits EGFR kinase, HER2 kinase and DHFR with IC50s of 0.45, 0.244 and 5.669 μM, respectively. EGFR/HER2-IN-8 shows anticancer activity against several cancer cell lines with high safety profile and selectivity indices. EGFR/HER2-IN-8 can be used for the research of cancer[1].

IC50 & Target

IC50: 0.45 μM (EGFR kinase), 0.244 μM (HER2 kinase), 5.669 μM (DHFR)[1]

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HCT-116 IC50
9.23 μM
Compound: 34
Antiproliferative activity against human HCT-116 cells after 72 hrs by MTT assay
Antiproliferative activity against human HCT-116 cells after 72 hrs by MTT assay
[PMID: 35964425]
HeLa IC50
13.02 μM
Compound: 34
Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay
Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay
[PMID: 35964425]
HepG2 IC50
7.34 μM
Compound: 34
Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay
Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay
[PMID: 35964425]
MCF7 IC50
5.19 μM
Compound: 34
Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay
Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay
[PMID: 35964425]
PC-3 IC50
18.5 μM
Compound: 34
Antiproliferative activity against human PC-3 cells after 72 hrs by MTT assay
Antiproliferative activity against human PC-3 cells after 72 hrs by MTT assay
[PMID: 35964425]
WI-38 IC50
67.23 μM
Compound: 34
Antiproliferative activity against human WI-38 cells after 72 hrs by MTT assay
Antiproliferative activity against human WI-38 cells after 72 hrs by MTT assay
[PMID: 35964425]
体外研究
(In Vitro)

EGFR/HER2-IN-8 (0-100 μM; 72 h) shows highly potent anticancer activity to HepG2, MCF 7, HCT-116, PC-3 and Hela cell lines and exhibits selective cytotoxicity against cancer cell lines rather than normal cell line[1].

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

Cell Cytotoxicity Assay[1]

Cell Line: HepG2 hepatocellular carcinoma, MCF 7 breast cancer, HCT-116 colorectal carcinoma, PC-3 prostate, Hea cervical epithelioid carcinoma cell lines and WI-38 fetal lung fibroblast cells
Concentration: 0-100 μM
Incubation Time: 72 hours
Result: Exibited more potent cytotoxicity than SOR towards HepG2, MCF 7, HCT-116, PC-3 and Hela cell lines with IC50s of 7.34, 5.19, 9.23, 18.5 and 13.02 μM, respectively. Showed weak cytotoxic activity against WI-38 cell line with an IC50 value of 67.25 μM, and possessed best selectivity indices towards MCF-7 breast cancer cell line.
分子量

328.39

Formula

C16H16N4O2S

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/HER2-IN-8
目录号:
HY-151161
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