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Tesevatinib

Catalog No. TQ0166   CAS 781613-23-8
Synonyms: KD-019, XL-647, EXEL-7647

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 products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
Tesevatinib Chemical Structure
Tesevatinib, CAS 781613-23-8
Pack Size Availability Price/USD Quantity
1 mg In stock $ 109.00
2 mg In stock $ 158.00
5 mg In stock $ 249.00
10 mg In stock $ 482.00
25 mg In stock $ 789.00
50 mg In stock $ 1,080.00
1 mL * 10 mM (in DMSO) In stock $ 269.00
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Purity: 97.89%
Purity: 97.89%
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Biological Description
Chemical Properties
Storage & Solubility Information
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).
Targets&IC50 EGFR:0.3 nM, Flt4:8.7 nM, KDR:1.5 nM, ErbB2:16 nM
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.
Synonyms KD-019, XL-647, EXEL-7647
Molecular Weight 491.39
Formula C24H25Cl2FN4O2
CAS No. 781613-23-8

Storage

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

Solubility Information

DMSO: 30 mg/mL (61.05 mM)

TargetMolReferences and Literature

1. Gendreau SB, et al. Inhibition of the T790M gatekeeper mutant of the epidermal growth factor receptor by EXEL-7647. Clin Cancer Res. 2007 Jun 15;13(12):3713-23.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Active Compound Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Tyrosine Kinase Inhibitor Library ReFRAME Related Library Anti-Cancer Compound Library Kinase Inhibitor Library Bioactive Compound Library Clinical Compound Library Anti-Breast Cancer Compound Library

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BRD7389 CHMFL-FLT3-122 Tandutinib SKLB4771 AXL-IN-13 (E/Z)-Zotiraciclib Pexidartinib Sitravatinib

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Keywords

Tesevatinib 781613-23-8 Angiogenesis JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR VEGFR FLT Ephrin Receptor EXEL7647 HER1 XL647 Inhibitor KD-019 Vascular endothelial growth factor receptor XL-647 KD019 Epidermal growth factor receptor KD 019 EXEL-7647 ErbB-1 XL 647 EXEL 7647 inhibit inhibitor

 

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