1000599-06-3
Chemical Structure
Tesevatinib tosylate
Synonym(s): XL-647 tosylate; EXEL-7647 tosylate; KD-019tosylate
- CAS No.: 1000599-06-3
- Formula:C31H33Cl2FN4O5S
- Molecular Weight:663.59
IUPAC Name: N-(3,4-dichloro-2-fluorophenyl)-6-methoxy-7-(((3aR,5r,6aS)-2-methyloctahydrocyclopenta[c]pyrrol-5-yl)methoxy)quinazolin-4-amine 4-methylbenzenesulfonate
InChIKey: GQLLAIBEWDUUBQ-QIYAQLFNSA-N
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.OS(=O)(C6=CC=C(C)C=C6)=O
Biological Activity: Tesevatinib (XL-647) tosylate is an orally available, blood-brain barrier-penetrant inhibitor of the epidermal growth factor receptor (EGFR). Tesevatinib tosylate significantly reduces cellular viability, with IC50 values of 11 nM and 102 nM in GBM12 and GBM6, respectively. Tesevatinib tosylate also inhibits HER2 (IC50=16.1 nM), VEGFR2 (IC50=1.5 nM), and Src (IC50=10.3 nM). Tesevatinib tosylate can inhibit tumor proliferation and exhibits antitumor activity[1][2].
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Tesevatinib tosylate | Tesevatinib (XL-647) tosylate is an orally available, blood-brain barrier-penetrant inhibitor of the epidermal growth factor receptor (EGFR). Tesevatinib tosylate significantly reduces cellular viability, with IC50 values of 11 nM and 102 nM in GBM12 and GBM6, respectively. Tesevatinib tosylate also inhibits HER2 (IC50=16.1 nM), VEGFR2 (IC50=1.5 nM), and Src (IC50=10.3 nM). Tesevatinib tosylate can inhibit tumor proliferation and exhibits antitumor activity. | |||||||||||||||||||||
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- [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. [Content Brief]
- [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. [Content Brief]
Keywords
