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CAS No. : 1776112-90-3
MCE 国际站:Mavelertinib
产品活性:Mavelertinib 是一种选择性的,口服有效的且不可逆的 EGFR 酪氨酸激酶抑制剂 (EGFR TKI),对 Del,L858R 和双重突变体 T790M/L858R 和 T790M/Del 的 IC50 值分别为 5、4、12 和 3 nM。Mavelertinib 可用于非小细胞肺癌 (NSCLC) 的研究。
研究领域:JAK/STAT Signaling | Protein Tyrosine Kinase/RTK
作用靶点:EGFR
In Vitro: Mavelertinib exhibits selectivity over wild-type EGFR (IC50=307 nM).
Mavelertinib (10 μM) exhibits less than 50% effect or inhibition against all nonkinase targets.
Mavelertinib inhibits the hERG26 current with an IC50 > 100 μM.
In Vivo: Mavelertinib exhibits low to moderate oral bioavailability (mouse 60%, rat 11%, dog 66%) following oral administration (mouse 1, rat 30, dog 3 mg/kg).
Mavelertinib exhibits short plasma half-lives (mouse 0.56, rat 0.28, dog 1.3 h) due to moderate to high plasma clearance (mouse 53, rat 49, dog 12 mL/min/kg) and low steady-state volume of distribution (mouse 1.48, rat 0.66, dog 0.94 L/kg) following intravenous administration (1 mg/kg to mouse, rat and dog).
相关产品:Covalent Screening Library Plus | Drug Repurposing Compound 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 | Drug Repurposing Compound Library | Covalent Screening Library | Differentiation Inducing Compound Library | Orally Active Compound Library | Anti-Hepatitis C Virus 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 | Cysteine Targeted Covalent Library | Highly Selective Inhibitors 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 | AV-412 free base | Falnidamol | EGFR/ErbB-2/ErbB-4 inhibitor-2 | Trastuzumab | EGFR-IN-58 | Naquotinib | MS9449
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