AV-412

AV-412 (MP412) is an EGFR inhibitor with IC 50 s of 0.75, 0.5, 0.79, 2.3, 19 nM for EGFR , EGFR L858R , EGFR T790M , EGFR L858R/T790M and ErbB2, respectively. In Vitro 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:EGFR 0.75 nM (IC 50 ) EGFR L858R 0.5 nM (IC 50 ) EGFR T790M 0.79 nM (IC 50 ) EGFR L858R/T790M 2.3 nM (IC 50 ) ErbB2 19 nM (IC 50 )

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