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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，EGFR^L858R，EGFR^T790M，EGFR^L858R/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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