AV-412_MP-412_EGFR-HER2_CAS号451493-31-5说明书_AbMole中国

化学数据

分子量分子式CAS号储存条件

851.41

C27H28ClFN6O.2C7H8O3S451493-31-53年 -20°C 粉末状

溶解性（25°C）

DMSO 10 mMWater <1 mMEthanol <1 mM

生物活性

AV-412 is a second-generation, orally bioavailable dual EGFR/HER2 tyrosine kinase inhibitor. AV-412 possesses potential antineoplastic activity. AV-412 binds toand inhibits the epidermal growth factor receptor (EGFR) and the human epidermal growth factor receptor 2 (HER2), which may result in the inhibition of tumorgrowth and angiogenesis, and tumor regression in EGFR/HER2-expressing tumors. AV-412 may be active against EGFR/HER2-expressing tumor cells that areresistant to first-generation kinase inhibitors. EGFR and HER2 are receptor tyrosine kinases that play major roles in tumor cell proliferation and tumor

vascularization.In a study, at both 1 and 3 days following treatment, AV412-treated tumors revealed significantly more apoptotic regions compared with tumorsfrom mice treated with vehicle alone. Furthermore, the number of carcinoma cells expressing HER2 was decreased following treatment with AV-412. AV-412 isoriginally developed by AVEO Pharmaceuticals, Inc. The phase I clinical trials for AV-412 has been terminated in the treatment of tumor.

不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

小鼠

重量 (kg)体表面积 (m2)Km 系数

0.020.0073

动物 B的Km系数动物 A的Km系数

大鼠0.150.0256

兔1.80.1512

豚鼠0.40.058

仓鼠0.080.025

狗100.520

动物 A (mg/kg) = 动物 B (mg/kg) × 

例如，依据体表面积折算法，将白藜芦醇用于小鼠的剂量22.4 mg/kg 换算成大鼠的剂量，需要将22.4 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到白藜芦醇用于大鼠的等效剂量为11.2 mg/kg。