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EGFR/HER2-IN-4
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
EGFR/HER2-IN-4图片
CAS NO:1879071-89-2
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
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。
生物活性

EGFR/HER2-IN-4(compound 6d) is an orally active irreversible dual inhibitor. EGFR/HER2-IN-4 inhibitsEGFRwith anIC50value of 0.6 nM and demonstrates potentEGFRkinase inhibitory activities on L858R and T790M mutations. EGFR/HER2-IN-4 has potent antitumor efficacy in vivo and can be used for lungcancerresearch[1].

IC50& Target[1]

EGFR

0.6 nM (IC50)

HER2

 

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].

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].

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 Tmax4 h
Cmax92.32 μg/L
AUC0-a1030.9 μg/L*h
IV5 mg/kg
half life6.8 h
oral bioavailability46.1%
分子量

487.95

Formula

C24H27ClFN5O3

CAS 号

1879071-89-2

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.