Tesevatinib

• UNSPSC Description:

  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].

• Target Antigen:

  EGFR; Src; VEGFR

• Type:

  Reference compound

• Related Pathways:

  JAK/STAT Signaling;Protein Tyrosine Kinase/RTK

• Field of Research:

  Cancer

• Assay Protocol:

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

• 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 Weight:

  491.39

• 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.

• Shipping Conditions:

  Room Temperature

• CAS Number:

  781613-23-8