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Tesevatinib

Tesevatinib
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Purity:97.89%
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Tesevatinib

Catalog No. TQ0166Cas No. 781613-23-8
Tesevatinib (XL-647) is an orally available, multi-target tyrosine kinase inhibitor (IC50s: 0.3, 16, 1.5, 8.7, and 1.4 nM for EGFR, ErbB2, KDR, Flt4, and EphB4).
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
Pack SizePriceAvailabilityQuantity
1 mg$109In Stock
2 mg$158In Stock
5 mg$249In Stock
10 mg$482In Stock
25 mg$789In Stock
50 mg$1,080In Stock
1 mL x 10 mM (in DMSO)$269In Stock
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Product Introduction

Bioactivity
Description
Tesevatinib (XL-647) is an orally available, multi-target tyrosine kinase inhibitor (IC50s: 0.3, 16, 1.5, 8.7, and 1.4 nM for EGFR, ErbB2, KDR, Flt4, and EphB4).
In vitro
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).
Cell Research
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.
Animal Research
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.
AliasKD-019, XL-647, EXEL-7647
Chemical Properties
Molecular Weight491.39
FormulaC24H25Cl2FN4O2
Cas No.781613-23-8
Storage & Solubility Information
Storage Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
DMSO: 45 mg/mL (91.58 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.0350 mL10.1752 mL20.3504 mL101.7522 mL
5 mM0.4070 mL2.0350 mL4.0701 mL20.3504 mL
10 mM0.2035 mL1.0175 mL2.0350 mL10.1752 mL
20 mM0.1018 mL0.5088 mL1.0175 mL5.0876 mL
50 mM0.0407 mL0.2035 mL0.4070 mL2.0350 mL

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