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Tesevatinib

CAS No. : 781613-23-8

MCE 站：Tesevatinib

产品活性：Tesevatinib (XL-647; EXEL-7647; KD-019) 是口服可用的多靶点酪氨酸激酶抑制剂; 抑制 EGFR，ErbB2，KDR，Flt4 和 EphB4 激酶活性的 IC₅₀ 值分别为 0.3，16，1.5，8.7，和1.4 nM。

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

作用靶点：EGFR  |  VEGFR  |  Ephrin Receptor

In Vitro: Tesevatinib (XL-647) potently inhibits the EGF/ErbB2, VEGF, and ephrin RTK families. Tesevatinib (XL-647) is a reversible and ATP competitive inhibitor. Tesevatinib (XL-647) was inactive against a panel of 10 tyrosine kinases (including the insulin and the insulin-like growth factor-1 receptor) and 55 serine-threonine kinases (including cyclin-dependent kinases, stress-activated protein kinases, and protein kinase C isoforms). Tesevatinib (XL-647) inhibits cellular proliferation and EGFR pathway activation in the erlotinib-resistant H1975 cell line that harbors a double mutation (L858R and T790M) in the EGFR gene. In A431 cells, Tesevatinib (XL-647) reduces cell viability with IC₅₀ values of 13 nM.

In Vivo: Tesevatinib (XL-647) shows potent and long-lived inhibition of the WT EGFR in vivo. Tesevatinib (XL-647) substantially inhibits the growth of H1975 xenograft tumors and reduces both tumor EGFR signaling and tumor vessel density.

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  |  Reprogramming 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  |  Anti-Blood Cancer Compound Library  |  Gefitinib  |  Trastuzumab  |  Erlotinib  |  Cetuximab  |  AG490  |  Bevacizumab  |  Sunitinib  |  Semaxinib  |  Genistein  |  AG-1478  |  SU 5402  |  PD173074  |  Pertuzumab  |  BI-4020  |  5Z-7-Oxozeaenol  |  Cediranib  |  SAR131675  |  Gandotinib  |  NSC 228155  |  GW806742X  |  Tanshi IIA  |  PF-03814735  |  NVP-BHG712  |  Pelitinib  |  Mubritinib  |  TX1-85-1  |  Canertinib  |  Vatalanib dihydrochloride

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