Tesevatinib

Tesevatinib (XL-647) is an orally available, blood-brain barrier-penetrant inhibitor of the epidermal growth factor receptor (EGFR) . Tesevatinib significantly reduces cellular viability, with IC50 values of 11 nM and 102 nM in GBM12 and GBM6, respectively. Tesevatinib also inhibits HER2 (IC50=16.1 nM), VEGFR2 (IC50=1.5 nM), and Src (IC50=10.3 nM) . Tesevatinib can inhibit tumor proliferation and exhibits antitumor activity[1][2].

Product Specifications

CAS Number

[781613-23-8]

Product Name Alternative

XL-647; EXEL-7647; KD-019

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

EGFR; Src; VEGFR

Type

Reference compound

Related Pathways

JAK/STAT Signaling; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/XL-647.html

Purity

99.41

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

[H][C@@]12[C@@](C[C@@H](COC3=CC4=C(C(NC5=C(F)C(Cl)=C(Cl)C=C5)=NC=N4)C=C3OC)C2)([H])CN(C)C1

Molecular Formula

C24H25Cl2FN4O2

Molecular Weight

491.39

Precautions

H302, H315, H319, H335

References & Citations

[1]Sani H Kizilbash, et al. In Vivo Efficacy of Tesevatinib in EGFR-Amplified Patient-Derived Xenograft Glioblastoma Models May Be Limited by Tissue Binding and Compensatory Signaling. Mol Cancer Ther. 2021 Jun;20 (6) :1009-1018.|[2]Steven B Gendreau, 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.