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EGFR/HER2-IN-5
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-5图片
CAS NO:1879071-97-2
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-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。
生物活性

EGFR/HER2-IN-5 (compound 6h) is an orally active irreversible dual inhibitor. EGFR/HER2-IN-5 inhibitsEGFRwith anIC50value of 1.01 nM and demonstrates potentEGFRkinase inhibitory activities on L858R and T790M mutations. EGFR/HER2-IN-5 has potent antitumor efficacy in vivo and can be used for lungcancerresearch[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].

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].

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 Tmax8 h
Cmax39.4 μg/L
AUC0-a780 μg/L*h
IV5 mg/kg
half life4.9 h
oral bioavailability28.8%
分子量

577.07

Formula

C30H33ClN6O4

CAS 号

1879071-97-2

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.