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Tesevatinib (tosylate)

CAT: 0804-HY-13314ASize: 1 EachDry Ice: NoHazardous: No
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Description
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].
CAS Number
1000599-06-3
Product Name Alternative
XL-647 (tosylate) ; EXEL-7647 (tosylate) ; KD-019 (tosylate)
UNSPSC
12352005
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/tesevatinib-tosylate.html
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
Molecular Formula
C31H33Cl2FN4O5S
Molecular Weight
663.59
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
Scientific Category
Reference compound1
Clinical Information
Phase 3
Isoform
VEGFR2/KDR/Flk-1

Chemical Information

Tesevatinib tosylate

Tesevatinib Tosylate is the tosylate salt form of tesevatinib, an orally bioavailable small-molecule receptor tyrosine kinase (RTK) inhibitor, with potential antineoplastic activity. Upon administration, tesevatinib binds to and inhibits several tyrosine receptor kinases that play major roles in tumor cell proliferation and tumor vascularization, including epidermal growth factor receptor (EGFR; ERBB1), epidermal growth factor receptor 2 (HER2; ERBB2), vascular endothelial growth factor receptor (VEGFR), and ephrin B4 (EphB4). This may result in the inhibition of tumor growth and angiogenesis, and tumor regression.

CAS Number1000599-06-3
PubChem CID71301378
IUPAC Name7-[[(3aS,6aR)-2-methyl-3,3a,4,5,6,6a-hexahydro-1H-cyclopenta[c]pyrrol-5-yl]methoxy]-N-(3,4-dichloro-2-fluorophenyl)-6-methoxyquinazolin-4-amine;4-methylbenzenesulfonic acid
Molecular FormulaC31H33Cl2FN4O5S
Molecular Weight663.6
Topological Polar Surface Area122
Hydrogen Bond Donor Count2
Hydrogen Bond Acceptor Count10
Rotatable Bond Count7
Heavy Atom Count44
Formal Charge0
Complexity858
SMILES
CC1=CC=C(C=C1)S(=O)(=O)O.CN1C[C@H]2CC(C[C@H]2C1)COC3=C(C=C4C(=C3)N=CN=C4NC5=C(C(=C(C=C5)Cl)Cl)F)OC
InChI
InChI=1S/C24H25Cl2FN4O2.C7H8O3S/c1-31-9-14-5-13(6-15(14)10-31)11-33-21-8-19-16(7-20(21)32-2)24(29-12-28-19)30-18-4-3-17(25)22(26)23(18)27;1-6-2-4-7(5-3-6)11(8,9)10/h3-4,7-8,12-15H,5-6,9-11H2,1-2H3,(H,28,29,30);2-5H,1H3,(H,8,9,10)/t13?,14-,15+;
InChIKey
GQLLAIBEWDUUBQ-XZPOUAKSSA-N
Chemical Structure
2D Structure
2D structure of Tesevatinib tosylate
CAS: 1000599-06-3
CID: 71301378
Formula: C31H33Cl2FN4O5S
MW: 663.6
Interactive 3D Structure
Loading 3D structure...
View on PubChemRaw 3D data
Computed Properties
PropertyValue
Molecular Weight663.6
Hydrogen Bond Donor Count2
Hydrogen Bond Acceptor Count10
Rotatable Bond Count7
Exact Mass662.1532749
Monoisotopic Mass662.1532749
Topological Polar Surface Area122 Ų
Heavy Atom Count44
Formal Charge0
Complexity858
Isotope Atom Count0
Defined Atom Stereocenter Count2
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently-Bonded Unit Count2
Compound Is CanonicalizedYes

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