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Angiogenesis EGFR Tesevatinib

Tesevatinib

Catalog No. TQ0166   CAS 781613-23-8
Synonyms: XL-647, KD-019
Purity 98.00% Datasheet

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).

Tesevatinib, CAS 781613-23-8
Pack Size Availability Price/USD Quantity
25 mg Inquiry 1126.00
50 mg Inquiry 1724.00
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Purity 98.00%
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
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 XL-647, KD-019
Purity 98.00%
Appearance solid
Molecular Weight 491.39
Formula C24H25Cl2FN4O2
CAS No. 781613-23-8

Storage

-20℃ 3 years powder

-80℃ 2 years in solvent

Solubility Information

:

DMSO: ≥30mg/mL(61.05 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References 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.

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