EGFR/HER2-IN-5

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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。

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 T_max	8 h
C_max	39.4 μg/L
AUC_0-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

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.