Tesevatinib tosylate
Based on 4 publication(s) in Google Scholar
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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- CAS No.: 1000599-06-3
- Formula: C31H33Cl2FN4O5S
- Molecular Weight:663.59
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Tesevatinib tosylate
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Biological Activity
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HER2 16.1 nM (IC50) |
VEGFR2 1.5 nM (IC50) |
Chemical Information
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CAS No. 1000599-06-3
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Molecular Weight 663.59
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Formula C31H33Cl2FN4O5S
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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
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Synonyms
XL-647 tosylate; EXEL-7647 tosylate; KD-019tosylate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (4)
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Journal Impact Factor
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Most Recent
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Science
2017 Dec 1;358(6367):eaan4368. PMID: 29191878 -
Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
Cell Rep
2023 Dec 26;42(12):113431. PMID: 38039961 -
Purity & Documentation
References
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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