2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK Apoptosis
  3. EGFR Apoptosis
  4. EGFR/HER2-IN-6

EGFR/HER2-IN-6 (compound 43) 是 EGFR/HER2 和 DHFR 的抑制剂。EGFR/HER2-IN-6 抑制 EGFR 和 HER2 激酶以及 DHFR，其 IC50 值分别为 0.122，0.078 和 0.585 μM。EGFR/HER2-IN-6 对多种肿瘤细胞具有较高的抗癌活性，以及有较高的安全性和选择性指标。EGFR/HER2-IN-8 可用于癌症的研究。

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EGFR/HER2-IN-6 Chemical Structure

EGFR/HER2-IN-6 Chemical Structure

CAS No. : 2820126-50-7

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EGFR/HER2-IN-6 相关抗体

Top Publications Citing Use of Products

查看 EGFR 亚型特异性产品:

查看所有亚型
EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

EGFR/HER2-IN-6 (compound 43) is an EGFR/HER2 and DHFR inhibitor. EGFR/HER2-IN-6 inhibits EGFR kinase, HER2 kinase and DHFR with IC50s of 0.122, 0.078 and 0.585 μM, respectively. EGFR/HER2-IN-6 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: 0.122 μM (EGFR kinase), 0.078 μM (HER2 kinase), 0.585 μM (DHFR)[1]
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HCT-116 IC50
16.18 μM
Compound: 43
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
9.43 μM
Compound: 43
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
12.18 μM
Compound: 43
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
2.37 μM
Compound: 43
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
18.39 μM
Compound: 43
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
36.84 μM
Compound: 43
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-6 (0-100 μM; 72 h) shows remarkable broad spectrum cytotoxic potency, and the cytotoxic potency against MCF7 cells is more potent than SOR[1].
EGFR/HER2-IN-6 (0-20 μM; 0-48 h) affects cell cycle and indeces apoptosis of MCF-7 cells[1].

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

EGFR/HER2-IN-6 相关抗体:

Cell Cytotoxicity Assay[1]

Cell Line: HepG2 hepatocellular carcinoma, MCF7 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: Exhibited cytotoxic potency to HepG2, MCF7, HCT-116, PC-3 and Hela cell lines with IC50s of 12.18, 2.37, 16.18, 18.39 and 9.43 μM. Showed a lower cytotoxic potency to WI-38 normal cell line with an IC50 value of 36.84 μM.

Apoptosis Analysis[1]

Cell Line: MCF-7 breast cancer cell line
Concentration: 0-20 μM
Incubation Time: 0-48 hours
Result: Through arrested cell cycle at G1/S and G1 phases and induced apoptosis in MCF-7 cells rather than necrosis to achieve anti-breast cancer activity.
体内研究
(In Vivo)

EGFR/HER2-IN-6 (10 mg/kg; i.p. once per day for 20days) shows anti-breast cancer activity in mice[1].

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

Animal Model: 8-week-old swiss albino female mice[1]
Dosage: 10 mg/kg
Administration: Intraperitoneal injection; 10 mg/kg once per day; for 20 days
Result: Decreased tumor volume 65.3% and reduced body weight 7.4% after 20 days of treatment.
分子量

387.46

Formula

C18H21N5O3S
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

EGFR/HER2-IN-6 相关分类

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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.

Keywords:

EGFR/HER2-IN-62820126-50-7EGFRApoptosisEpidermal growth factor receptorErbB-1HER1thiazoleMCF-7anticancerbroad spectrum cytotoxicSORHelaHepG2HCT-116PC-3Inhibitorinhibitorinhibit

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