781613-23-8
Chemical Structure
Tesevatinib
Synonym(s): XL-647; EXEL-7647; KD-019
- CAS No.: 781613-23-8
- Formula:C24H25Cl2FN4O2
- Molecular Weight:491.39
IUPAC Name: N-(3,4-dichloro-2-fluorophenyl)-6-methoxy-7-(((3aR,5r,6aS)-2-methyloctahydrocyclopenta[c]pyrrol-5-yl)methoxy)quinazolin-4-amine
InChIKey: HVXKQKFEHMGHSL-QKDCVEJESA-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
Biological Activity: 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].
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Tesevatinib | 99.41% | 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. | ||||||||||||||||||||
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Tesevatinib (Standard) | ≥98% | Tesevatinib (Standard) is the analytical standard of Tesevatinib. This product is intended for research and analytical applications. 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. | ||||||||||||||||||||
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- [1]. 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]
- [2]. 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]
Keywords
