2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  3. EGFR
  4. EGFR/HER2-IN-5

EGFR/HER2-IN-5 (化合物6h) 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-5 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-5 Chemical Structure

EGFR/HER2-IN-5 Chemical Structure

CAS No. : 1879071-97-2

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EGFR/HER2-IN-5 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-5 (compound 6h) is an orally active irreversible dual inhibitor. EGFR/HER2-IN-5 inhibits EGFR with an IC50 value of 1.01 nM and demonstrates potent EGFR kinase inhibitory activities on L858R and T790M mutations. EGFR/HER2-IN-5 has potent antitumor efficacy in vivo and can be used for lung cancer research[1].

IC50 & Target

EGFR

0.6 nM (IC50)

HER2

0.6 nM (IC50)

体外研究
(In Vitro)

EGFR/HER2-IN-5 (compound 6h) (0-10 μM, 72 hours) shows good anti-proliferative activity against lung cancer, where the effect against mutant lung cancer HCC 827 is superior to that of NCI-H1975 and A431[1].

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

EGFR/HER2-IN-5 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 hour
Result: Inhibited NCI-H1975 cells, HCC 827 cells, A431 cells with the IC50values of 60.6 nM, 1.2 nM and 288.3 nM respectively.
体内研究
(In Vivo)

EGFR/HER2-IN-5 (compound 6h) (oral gavage; 99.5 mg/kg, 24.9 mg/kg, 6.2 mg/kg; every other day or every day; 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: 99.5 mg/kg, 24.9 mg/kg, 6.2 mg/kg
Administration: Oral gavage; 99.5 mg/kg and 24.9 mg/kg for every other day for 25 days; 6.2 mg/kg for every day for 25 days
Result: Inhibited 84.11% of tumor xenografts growth at 99.5 mg/kg, 65.72% at 24.9 mg/kg, and 47% at 6.2 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-5 (compound 6h) oral (10 mg/kg)
Parameter
Oral Tmax 8 h
Cmax 39.4 μg/L
AUC0-a 780 μg/L*h
IV 5 mg/kg
half life 4.9 h
oral bioavailability 28.8%
分子量

577.07

Formula

C30H33ClN6O4
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-5 相关分类

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Keywords:

EGFR/HER2-IN-51879071-97-2EGFREpidermal growth factor receptorErbB-1HER1HER2Lung cancerNCI-H1975NSCLCXenograftInhibitorinhibitorinhibit

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