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Tesevatinib

Tesevatinib

Item no.	HY-13314-1mg
Manufacturer	MedChem Express
CASRN	781613-23-8
Amount	1 mg
Quantity options	10 mM/1 mL 10 mg 1 mg 50 mg 5 mg
Category	Inhibitors & Compound Libraries Small Molecules
Type	Inhibitors
Specific against	other
Purity	99.41
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.
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
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	XL-647,EXEL-7647,KD-019
Shipping Condition	Room temperature
Available
Manufacturer - Type	Reference compound
Manufacturer - Applications	Cancer-Kinase/protease
Manufacturer - Targets	EGFR; Src; VEGFR
Shipping Temperature	Room Temperature
Storage Conditions	-20°C, 3 years; 4°C, 2 years (Powder)
Molecular Weight	491.39
Product 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].
Manufacturer - Research Area	Cancer
Solubility	DMSO : 100 mg/mL (ultrasonic)
Manufacturer - Pathway	JAK/STAT Signaling; Protein Tyrosine Kinase/RTK
Clinical information	Phase 3
Isoform	EGFR/ErbB1/HER1; ErbB2/HER2; VEGFR2/KDR/Flk-1; VEGFR3/Flt-4

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