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CAS No. : 451492-95-8
MCE 国际站:AV-412 free base
产品活性:AV-412 free base (MP-412 free base) 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 | Anti-Obesity Compound Library | Angiogenesis-Related Compound Library | Anti-Liver Cancer Compound Library | Anti-Colorectal Cancer Compound Library | Anti-Prostate Cancer Compound Library | Cancer Stem Cells Compound Library | Heterocyclic Compound Library | Membrane Protein-targeted Compound Library | Membrane Receptor-targeted Compound Library | EGFR/HER2/CDK9-IN-2 | Lapatinib ditosylate | BMS-690514 | Erlotinib-d6 hydrochloride | EGFR/CDK2-IN-1 | JBJ-04-125-02 | EGFR-IN-22 | EGFR-IN-34 | Epertinib | Ponezumab | Erlotinib Hydrochloride | EGFR-IN-36 | EGFR-IN-62 | Genistein | Panitumumab (anti-EGFR) | Lirafugratinib | Lapatinib-d7 dihydrochloride | (E/Z)-CP-724714 | TAS0728 | Rezivertinib | Tucatinib hemiethanolate | Osimertinib mesylate | Falnidamol | EGFR/ErbB-2/ErbB-4 inhibitor-2 | Trastuzumab | EGFR-IN-58 | Naquotinib | MS9449
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货号: HY-10346A
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