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Tesevatinib

Catalog No. TQ0166 CAS 781613-23-8

Synonyms: EXEL-7647, XL-647, KD-019

Tesevatinib 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).

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Tesevatinib, CAS 781613-23-8

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Tesevatinib 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	EXEL-7647, XL-647, KD-019
Molecular Weight	491.39
Formula	C24H25Cl2FN4O2
CAS No.	781613-23-8

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 30 mg/mL (61.05 mM)

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

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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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Tesevatinib 781613-23-8 JAK/STAT信号通路蛋白酪氨酸激酶血管生成 EGFR Ephrin Receptor FLT VEGFR XL-647 XL647 EXEL 7647 KD019 HER1 Inhibitor EXEL-7647 KD 019 Vascular endothelial growth factor receptor Epidermal growth factor receptor ErbB-1 XL 647 EXEL7647 KD-019 inhibit inhibitor

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