Molecular Formula | C41H44ClFN6O7S2 |
Molar Mass | 851.4054632 |
Solubility | DMSO: ≥ 28 mg/mL |
Storage Condition | -20℃ |
In vitro study | AV-412 inhibits autophosphorylation of EGFR and ErbB2 with IC 50 of 43 and 282 nM, respectively. AV-412 also inhibits epidermal growth factor (EGF)-dependent cell proliferation with an IC 50 of 100 nM. AV-412 abrogates EGFR signaling in the gefitinib-resistant H1975 cell line, which harbors a double mutation of L858R and T790M in EGFR. |
In vivo study | In animal studies using cancer xenograft models, AV-412 (30 mg/kg) demonstrates complete inhibition of tumor growth of the A431 and BT-474 cell lines, which overexpress EGFR and ErbB2, respectively. AV-412 suppresses autophosphorylation of EGFR and ErbB2 at the dose corresponding to its antitumor efficacy. When various dosing schedules are applied, AV-412 shows significant effects with daily and every-other-day schedules, but not with a once-weekly schedule, suggesting that frequent dosing is preferable for this compound. Furthermore, AV-412 shows a significant antitumor effect on the ErbB2-overexpressing breast cancer KPL-4 cell line, which is resistant to gefitinib. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.175 ml | 5.873 ml | 11.745 ml |
5 mM | 0.235 ml | 1.175 ml | 2.349 ml |
10 mM | 0.117 ml | 0.587 ml | 1.175 ml |
5 mM | 0.023 ml | 0.117 ml | 0.235 ml |