Product Introduction
Bioactivity


英文名: Tesevatinib

描述: Tesevatinib (XL-647) 是一種口服的多靶點酪氨酸激酶抑制劑，對 EGFR、ErbB2、KDR、Flt4和 EphB4的 IC50值分別為 0.3、16、1.5、8.7和 1.4 nM。

細胞實驗: Growth inhibition of H1975 and A431 cells by increasing concentrations of Tesevatinib is determined by seeding 5000 cells per well in 96-well plates. The following day, cells are washed once with low-serum RPMI 1640 (0.1% fetal bovine serum, 1% nonessential amino acids, and 1% penicillin/streptomycin), after which 90 μL of the low-serum RPMI 1640 is added. Tesevatinib is diluted to 10 times the test concentrations and 10 μL are added to triplicate wells for a 72-h incubation. Cell viability is determined.

動物實驗: Tumor-bearing mice are given either Tesevatinib, erlotinib, or gefitinib at 100 mg/kg and tumors are harvested 1 to 72 h later. Half an hour before the respective time point, EGF (50 μg/mouse) is given via i.v. bolus injection with tumors dissected 30 min later and tumor extracts are prepared by homogenization in 10 volumes of ice-cold lysis buffer. Lysates are clarified by centrifugation and EGFR tyrosine phosphorylation levels are determined by ELISA.

體外活性: Tesevatinib 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 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 reduces cell viability (IC50: 13 nM).

存儲條件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 45 mg/mL (91.58 mM)


關(guān)鍵字: EXEL7647 | HER1 | XL647 | Ephrin Receptor | Inhibitor | VEGFR | Vascular endothelial growth factor receptor | KD019 | Epidermal growth factor receptor | KD 019 | EGFR | ErbB-1 | Tesevatinib | XL 647 | EXEL 7647 | inhibit

相關(guān)產(chǎn)品: (Rac)-JBJ-04-125-02 | EGFR-IN-9 | Tyrosine kinase-IN-7 | EGFR-IN-61 | Khellin | PD-161570 | Simotinib | Lapatinib ditosylate monohydrate | Icotinib Hydrochloride | Mutant EGFR inhibitor

相關(guān)庫: Drug Repurposing Compound Library | Cytokine Inhibitor Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | Tyrosine Kinase Inhibitor Library | Anti-Cancer Active Compound Library | Anti-Pancreatic Cancer Compound Library

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