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 to and inhibits the epidermal growth factor receptor (EGFR) and the human epidermal growth factor receptor 2 (HER2), which may result in the inhibition of tumor growth and angiogenesis, and tumor regression in EGFR/HER2-expressing tumors. AV-412 may be active against EGFR/HER2-expressing tumor cells that are resistant 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 tumors from mice treated with vehicle alone. Furthermore, the number of carcinoma cells expressing HER2 was decreased following treatment with AV-412. AV-412 is originally developed by AVEO Pharmaceuticals, Inc. The phase I clinical trials for AV-412 has been terminated in the treatment of tumor.

化学数据

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）

例如，依据体表面积折算法，将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量，需要将20 mg/kg 乘以小鼠的K_m系数（3），再除以大鼠的K_m系数（6），得到化合物用于大鼠的等效剂量为10 mg/kg。

储备液配制

以下数据基于产品分子量，对于特殊产品，请参照COA中的储备液配制条件和说明进行操作。