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Mobocertinib

CAS No. : 1847461-43-1

MCE 站：Mobocertinib

产品活性：Mobocertinib (TAK-788) 是一种有效的的，具有口服活性的 EGFR 和 HER2 突变的抑制剂，包括外显子 20 的插入，并且选择性高于 WT EGFR。具有抗肿瘤活性。

研究领域：JAK/STAT Signaling  |  Protein Tyrosine Kinase/RTK

作用靶点：EGFR

In Vitro: Mobocertinib (TAK-788) inhibits all 14 mutant variants of EGFR (IC₅₀s=2.4-22 nM), and all 6 mutant variants of HER2 (IC₅₀s=2.4-26 nM), more potently than it inhibited WT EGFR (IC₅₀=35 nM), including all 8 variants with exon 20 activating insertions.

In Vivo: In mice implanted with a patient-derived tumor containing an EGFR exon 20 activating insertion, or with engineered Ba/F3 cells containing a HER2 exon 20 activating insertion, once daily oral dosing of Mobocertinib induced regression of tumors at doses that were well tolerated (30-100 mg/kg).

相关产品：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  |  Differentiation Inducing Compound Library  |  Orally Active 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  |  AV-412

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