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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 |
| Related EGFR/HER2 Products |
|---|
| Nimotuzumab
Nimotuzumab (Nimotuzumab) is the first humanized monoclonal antibody targeting epidermal growth factor receptor (EGFR). Nimotuzumab has cytolytic effects on target tumors through its ability to induce antibody-dependent cell-mediated cytotoxicity (ADCC) and complement dependent cytotoxicity (CDC). Nimotuzumab failed to recognize mouse EGFR. |
| Matuzumab
Matuzumab (EMD 72000) is a humanized monoclonal antibody that binds tightly to EGFR. |
| AEE788
AEE788 (NVP-AEE788) is a novel multitargeted HER 1/2 and VEGFR 1/2 receptor family tyrosine kinases inhibitor with IC50 of 2, 6, 77, 59 nM for EGFR, ErbB2, KDR, and Flt-1. |
| Sapitinib (AZD8931)
AZD8931 (Sapitinib) is an equipotent, reversible inhibitor of Signaling by EGFR, ERBB2 (HER2), and ERBB3 with IC50 of 4, 3, 4 nM respectively. |
| Afatinib
Afatinib (BIBW 2992) is a novel irreversible dual EGFR and HER2 tyrosine kinase inhibitor. |
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