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Cabozantinib (hydrochloride)

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].

Product Specifications

CAS Number

[1817759-42-4]

Product Name Alternative

XL184 (hydrochloride) ; BMS-907351 (hydrochloride)

UNSPSC

12352005

Target

Apoptosis; c-Kit; c-Met/HGFR; FLT3; TAM Receptor; VEGFR

Type

Reference compound

Related Pathways

Apoptosis; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/cabozantinib-hydrochloride.html

Solubility

10 mM in DMSO

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

Molecular Formula

C28H25ClFN3O5

Molecular Weight

537.97

References & Citations

[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.

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

Launched

Isoform

Axl; VEGFR1/Flt-1; VEGFR2/KDR/Flk-1; VEGFR3/Flt-4

Citation 01

Virology. 2023 Aug:585:205-214.|Acta Pharmacol Sin. 2021 Jan;42 (1) :108-114.|Adv Healthc Mater. 2023 Dec;12 (31) :e2302046.|Am J Reprod Immunol. 2021 Mar;85 (3) :e13352.|Antioxidants (Basel) . 2021 Aug 24;10 (9) :1336.|Biochem Biophys Rep. 2020 Jan 17;21:100726.|Biochem Biophys Res Commun. 2024 Nov 19:734:150781.|Bioengineering (Basel) . 2025 Oct 19;12 (10) :1121.|Biomaterials. 2022 Oct:289:121800.|Biomed Chromatogr. 2020 Aug;34 (8) :e4862.|Biomed Chromatogr. 2023 Sep;37 (9) :e5685.|Biomed Chromatogr. 2024 May;38 (5) :e5833.|Biomedicines. 2020 Nov 28;8 (12) :547.|bioRxiv. 2023 Apr 14.|bioRxiv. 2024 November 03.|bioRxiv. 2025 May 21.|BMC Biol. 2024 Oct 1;22 (1) :222.|Br J Cancer. 2024 Aug;131 (3) :601-610.|Br J Pharmacol. 2025 May 21.|Cancer Discov. 2021 Jan;11 (1) :126-141.|Cancer Lett. 2019 Apr 10:447:105-114.|Cancers (Basel) . 2024 Jan 8, 16 (2), 269.|Cancers (Basel) . 2025 Sep 9;17 (18) :2950.|Cell Rep Med. 2025 Apr 2:102053.|Clin Transl Med. 2025 May;15 (5) :e70338. |Drug Des Devel Ther. 2018 Apr 30:12:1009-1017.|Eur J Drug Metab Pharmacokinet. 2021 Sep;46 (5) :625-635.|Eur J Pharmacol. 2025 Sep 15:1003:177942.|Exp Cell Res. 2020 Aug 1;393 (1) :112054.|Front Oncol. 2022 Jul 7;12:915319.|Fundam Clin Pharmacol. 2021 Oct;35 (5) :919-929.|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 Med Chem. 2025 Sep 25;68 (18) :19536-19553.|J Neurosci. 2020 Dec 9;40 (50) :9602-9616.|J Pharm Anal. 2021 Dec;11 (6) :799-807.|J Transl Med. 2023 Jan 9;21 (1) :9.|Mediators Inflamm. 2020 Oct 24;2020:1649453.|Mol Cancer Res. 2019 Feb;17 (2) :499-507. |Mol Cancer Ther. 2017 Nov;16 (11) :2387-2398.|Mol Med. 2025 May 27;31 (1) :209.|Patent. US20170349880A1.|Patent. US20220332731A1.|PLoS One. 2017 Sep 25;12 (9) :e0185321. |PLoS One. 2024 Nov 1;19 (11) :e0308647.|React Kinet Mech Cat. 07 January 2022.|Saudi Pharm J. 2023 Oct;31 (10) :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.
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