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Postion:Product Catalog >Tesevatinib
Tesevatinib
  • Tesevatinib

Tesevatinib NEW

Price $109 $158 $249
Package 1mg 2mg 5mg
Min. Order:
Supply Ability: 10g
Update Time: 2024-11-19

Product Details

Product Name: Tesevatinib CAS No.: 781613-23-8
Purity: 97.89% Supply Ability: 10g
Release date: 2024/11/19

Product Introduction

Bioactivity

NameTesevatinib
DescriptionTesevatinib (XL-647) is an oral, multi-targeted tyrosine kinase inhibitor with IC50 values ??of 0.3, 16, 1.5, 8.7, and 1.4 nM for EGFR, ErbB2, KDR, Flt4, and EphB4.
Cell ResearchGrowth 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.
Animal ResearchTumor-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.
In vitroTesevatinib (XL-647) potently inhibits the EGF/ErbB2, VEGF, and ephrin RTK families with IC50 values ??of 0.3, 16, 1.5, 8.7, and 1.4 nM for EGFR, ErbB2, KDR, and EphB4. [1]
In vivoMETHODS: To study the in vivo effects of Tesevatinib (XL-647) on T790M mutant EGFR, H1975 human tumor xenografts were established in female severe combined immunodeficient mice and administered Tesevatinib (XL-647) orally once daily (doses: 10, 30 and 100 mg/kg, 14 days) RESULTS Tesevatinib (XL-647) significantly inhibited tumor growth in a dose-dependent manner, with tumor growth inhibition rates of 33%, 66% and 92% respectively.[1] METHODS: Tesevatinib (XL-647) (7.5, 15 mg/kg, ip, daily) was treated in the well-characterized bpk mouse model of ARPKD, and efficacy and toxicity were evaluated in neonatal mice during postnatal development. RESULTS In vivo pharmacological inhibition of multiple kinase cascades by tesevatinib (XL-647) reduced phosphorylation of key mediators of cystogenesis: EGFR, ErbB2, c-Src, and KDR; decreased kinase activity resulted in significant reductions in renal and biliary disease in both the bpk and PCK models of ARPKD. Disease amelioration by tesevatinib (XL-647) was not associated with any overt toxicity. [2]
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility InformationDMSO : 45 mg/mL (91.58 mM)
KeywordsEXEL7647 | 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
Inhibitors RelatedGilteritinib | Osimertinib | Sorafenib | Lapatinib | Regorafenib | Erlotinib hydrochloride | Erlotinib | Neratinib | Genistein | Gefitinib | Pazopanib | Axitinib
Related Compound LibrariesBioactive Compound Library | Membrane Protein-targeted Compound Library | Tyrosine Kinase Inhibitor Library | Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Bioactive Compounds Library Max | Anti-Cancer Drug Library | Anti-Cancer Active Compound Library

Company Profile Introduction

Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers. TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.

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