EGFR/HER2-IN-4

立即咨询

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。

CAS NO:

1879071-89-2

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 T_max	4 h
C_max	92.32 μg/L
AUC_0-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

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.