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AV-412
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AV-412
CAS No. : 451493-31-5
MCE 站:AV-412
产品活性:AV-412 (MP412) 是 EGFR 抑制剂,抑制EGFR,EGFRL858R,EGFRT790M,EGFRL858R/T790M 和 ErbB2的 IC50 值分别为0.75,0.5,0.79,2.3,19 nM。
研究领域:JAK/STAT Signaling | Protein Tyrosine Kinase/RTK
作用靶点:EGFR
In Vitro: AV-412 inhibits autophosphorylation of EGFR and ErbB2 with IC50 of 43 and 282 nM, respectively. AV-412 also inhibits epidermal growth factor (EGF)-dependent cell proliferation with an IC50 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: 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.
相关产品:Covalent Screening Library Plus | Clinical Compound Library Plus | Bioactive Compound Library Plus | Immunology/Inflammation Compound Library | JAK/STAT Compound Library | Kinase Inhibitor Library | Protein Tyrosine Kinase Compound Library | Anti-Cancer Compound Library | Clinical Compound Library | Covalent Screening Library | Differentiation Inducing Compound Library | Anti-Hepatitis C Virus Compound Library | Anti-Breast Cancer Compound Library | Anti-Lung Cancer Compound Library | Anti-Pancreatic Cancer Compound Library | Gefitinib | Trastuzumab | Erlotinib | Cetuximab | AG490 | Genistein | AG-1478 | Pertuzumab | BI-4020 | NSC 228155 | Pelitinib | Mubritinib | TX1-85-1 | Canertinib | Butein | PD168393 | Daphnetin | EGFR-IN-7 | AEE788 | Chrysophanol | PD153035 | Tyrphostin 23 | Lavendustin A | Trastuzumab emtansine | BMS-599626 Hydrochloride | PD158780
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