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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.
| Molecular Weight | 851.41 |
| Formula | C27H28ClFN6O.2C7H8O3S |
| CAS Number | 451493-31-5 |
| Solubility (25°C) | DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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