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Product Description
– Cabozantinib hydrochloride is a potent and orally active inhibitor of VEGFR2 and MET, with IC50 values of 0.035 and 1.3 nM, respectively. Cabozantinib hydrochloride displays strong inhibition of KIT, RET, AXL, TIE2, and FLT3 (IC50=4.6, 5.2, 7, 14.3, and 11.3 nM, respectively). Cabozantinib hydrochloride shows antiangiogenic activity. Cabozantinib hydrochloride disrupts tumor vasculature and promotes tumor and endothelial cell apoptosis[1].
Web ID
– HY-13016A
Shipping
– Room temperature
Applications
– Cancer-Kinase/protease
Molecular Formula
– C28H25ClFN3O5
Citations
– Virology. 2023 Jun 21.|Acta Pharmacol Sin. 2021 Jan;42(1):108-114.|Adv Healthc Mater. 2023 Aug 21;e2302046.|Am J Reprod Immunol. 2021 Mar;85(3):e13352.|Antioxidants (Basel). 2021, 10(9), 1336.|Biochem Biophys Rep. 2020 Jan 17;21:100726.|Biomaterials. 16 September 2022.|Biomed Chromatogr. 2020 Aug;34(8):e4862.|Biomed Chromatogr. 2023 May 15;e5685.|Biomedicines. 2020 Nov 28;8(12):547.|bioRxiv. 2023 Apr 14.|Cancer Discov. 2021 Jan;11(1):126-141.|Cancer Lett. 2019 Apr 10;447:105-114.|Drug Des Devel Ther. 2018 Apr 30;12:1009-1017.|Eur J Drug Metab Pharmacokinet. 2021 Jul 18;1-11.|Exp Cell Res. 2020 Aug 1;393(1):112054.|Front Oncol. 2022 Jul 7;12:915319.|Fundam Clin Pharmacol. 2021 Feb 1.|Int J Mol Sci. 2022 Sep 14;23(18):10677.|Invest Ophthalmol Vis Sci. 2022 Dec 1;63(13):14.|J Cell Biochem. 2020 Mar;121(3):2343-2353.|J Med Chem. 2016 Jan 14;59(1):358-73.|J Neurosci. 2020 Dec 9;40(50):9602-9616.|J Pharm Anal. 2021 Jun 19.|J Transl Med. 2023 Jan 9;21(1):9.|Mediat Inflamm. 2020 Oct 24;2020:1649453.|Mol Cancer Res. 2019 Feb;17(2):499-507. |Mol Cancer Ther. 2017 Nov;16(11):2387-2398.|Patent. US20170349880A1.|Patent. US20220332731A1.|PLoS One. 2017 Sep 25;12(9):e0185321. |React Kinet Mech Cat. 07 January 2022.|Saudi Pharm J. 2023 Aug 24, 101756.|Sci Rep. 2019 Nov 12;9(1):16600.|Sci Transl Med. 2018 Jul 18;10(450):eaaq1093.|Spectrochim Acta A Mol Biomol Spectrosc. 2016 Apr 15;159:199-208.
References
– [1]Yakes FM, et al. Cabozantinib (XL184), a novel MET and VEGFR2 inhibitor, simultaneously suppresses metastasis, angiogenesis, and tumor growth. Mol Cancer Ther, 2011, 10(12), 2298-2308.|[2]You WK, et al. VEGF and c-Met blockade amplify angiogenesis inhibition in pancreatic islet cancer. Cancer Res, 2011, 71(14), 4758-4768.
CAS Number
– 1817759-42-4
Molecular Weight
– 537.97
SMILES
– O=C(C1(CC1)C(NC2=CC=C(F)C=C2)=O)NC3=CC=C(C=C3)OC4=C5C=C(OC)C(OC)=CC5=NC=C4.Cl
Clinical Information
– Launched
Research Area
– Cancer
Solubility
– 10 mM in DMSO
Target
– Apoptosis;c-Kit;c-Met/HGFR;FLT3;TAM Receptor;VEGFR
Isoform
– VEGFR1/Flt-1;VEGFR2/KDR/Flk-1;VEGFR3/Flt-4
Pathway
– Apoptosis;Protein Tyrosine Kinase/RTK
Product type
– Reference compound
Disclaimer: All products are for research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation.
