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

EGFR/HER2-IN-4 (化合物6d) 是一种具有口服活性的不可逆的双重抑制剂，其抑制 EGFR 活性IC50 值为 0.6 nM。对 L858R 和 T790M 突变表现出有效的 EGFR 激酶抑制活性。 EGFR/HER2-IN-4 在体内具有强大的抗肿瘤功效，可以用于肺癌研究。

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EGFR/HER2-IN-4

EGFR/HER2-IN-4 Chemical Structure

CAS No. : 1879071-89-2

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EGFR/HER2-IN-4 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-4(compound 6d) is an orally active irreversible dual inhibitor. EGFR/HER2-IN-4 inhibits EGFR with an IC50 value of 0.6 nM and demonstrates potent EGFR kinase inhibitory activities on L858R and T790M mutations. EGFR/HER2-IN-4 has potent antitumor efficacy in vivo and can be used for lung cancer research[1].

IC50 & Target[1]

EGFR

0.6 nM (IC50)

HER2

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A-431 IC50
1.52 nM
Compound: 1d
Antiproliferative activity against human A431 cells harboring wild-type EGFR after 72 hrs by CCK8 assay
Antiproliferative activity against human A431 cells harboring wild-type EGFR after 72 hrs by CCK8 assay
[PMID: 30600209]
HCC827 IC50
0.31 nM
Compound: 1d
Antiproliferative activity against human HCC827 cells harboring EGFR L858R mutant after 72 hrs by CCK8 assay
Antiproliferative activity against human HCC827 cells harboring EGFR L858R mutant after 72 hrs by CCK8 assay
[PMID: 30600209]
MDA-MB-453 IC50
0.62 nM
Compound: 1d
Antiproliferative activity against human MDA-MB-453 cells after 72 hrs by CCK8 assay
Antiproliferative activity against human MDA-MB-453 cells after 72 hrs by CCK8 assay
[PMID: 30600209]
NCI-H1975 IC50
12.2 nM
Compound: 1d
Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M mutant after 72 hrs by CCK8 assay
Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M mutant after 72 hrs by CCK8 assay
[PMID: 30600209]
体外研究
(In Vitro)

EGFR/HER2-IN-4 (compound 6d) (0-10 μM, 72 hours) shows well anti-proliferative activity against human non-small cell lung cancer cell lines NCI-H1975 (T790M), HCC 827 (L858R) and human epithelial carcinoma cell lines A431[1].

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

EGFR/HER2-IN-4 相关抗体:

Cell Proliferation Assay[1]

Cell Line: Human non-small cell lung cancer cell lines NCI-H1975 (T790M), HCC 827 (L858R), Human epithelial carcinoma cell lines A431
Concentration: 0-10 μM
Incubation Time: 72 hours
Result: Inhibited NCI-H1975 cells, HCC 827 cells, A431 cells with the IC50values of 107 nM,0.2 nM and 20 nM respectively.
体内研究
(In Vivo)

EGFR/HER2-IN-4 (compound 6d) (orally gavage; 5.1-81.4 mg/kg; for 25 days) has good cancer suppression effect in a dose-dependent manner in the constructed NCI-H1975 tumor xenograft model[1].

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

Animal Model: BALB/c nude mice, female, 6-7 weeks of age with NCI-H1975 tumor xenograft[1]
Dosage: 81.4mg/kg, 20.4mg/kg, 5.1mg/kg
Administration: Oral gavage; 81.4mg/kg and 20.4mg/kg for every other day for 25 days; 5.1mg/kg for every day for 25 days
Result: Inhibited 95.21% of tumor xenografts growth at 81.4mg/kg, 71.01% at 20.4 mg/kg, and 55.1% at 5.1 mg/kg in nude mice.
Animal Model: BALB/c nude mice, female, 6-7 weeks of age with NCI-H1975 tumor xenograft[1]
Dosage: 10 mg/kg
Administration: Oral gavage; 10 mg/kg; 25 days
Result: The pharmacokinetic parameters of EGFR/HER2-IN-4 oral (10 mg/kg)
Parameter
Oral Tmax 4 h
Cmax 92.32 μg/L
AUC0-a 1030.9 μg/L*h
IV 5 mg/kg
half life 6.8 h
oral bioavailability 46.1%
分子量

487.95

Formula

C24H27ClFN5O3
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-4 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-41879071-89-2EGFREpidermal growth factor receptorErbB-1HER1HER2Lung cancerNCI-H1975NSCLCXenograftInhibitorinhibitorinhibit

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