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Tesevatinib

CAT: 0804-HY-13314-01Size: 1 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-13314-01Size:1 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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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].
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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 3
Isoform
EGFR/ErbB1/HER1; ErbB2/HER2; VEGFR2/KDR/Flk-1; VEGFR3/Flt-4

Alternative Products

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BUP08766-01Tesevatinib
T201865-01Tesevatinib tosylate
MBS386423-01XL647 (Tesevatinib)
A11057-1XL647 (Tesevatinib) 1mg
A11057-2XL647 (Tesevatinib) 2mg
A11057-25XL647 (Tesevatinib) 25mg
A11057-10mM-DXL647 (Tesevatinib) 10mM * 1mL in DMSO

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