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Cabozantinib

Cabozantinib is a potent and orally active inhibitor of VEGFR2 and MET, with IC50 values of 0.035, and 1.3 nM, respectively. Cabozantinib displays strong inhibition of KIT, RET, AXL, TIE2, and FLT3 (IC50=4.6, 5.2, 7, 14.3, and 11.3 nM, respectively) . Cabozantinib shows antiangiogenic activity. Cabozantinib disrupts tumor vasculature and promotes tumor and endothelial cell apoptosis[1][2].

Product Specifications

CAS Number

[849217-68-1]

Product Name Alternative

XL184; BMS-907351

UNSPSC

12352005

Hazard Statement

H315, H319, H320

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.html

Purity

99.96

Solubility

DMSO : 25 mg/mL (ultrasonic)

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

Molecular Formula

C28H24FN3O5

Molecular Weight

501.51

Precautions

H315, H319, H320

References & Citations

[1]You WK, et al. VEGF and c-Met blockade amplify angiogenesis inhibition in pancreatic islet cancer. Cancer Res, 2011, 71 (14), 4758-4768.|[2]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.|[3]Fuse MA, et al. Combination Therapy With c-Met and Src Inhibitors Induces Caspase-Dependent Apoptosis of Merlin-Deficient Schwann Cells and Suppresses Growth of Schwannoma Cells. Mol Cancer Ther. Mol Cancer Ther. 2017 Nov;16 (11) :2387-2398.

Shipping Conditions

Room Temperature

Storage Conditions

4°C (Powder, protect from light)

Scientific Category

Reference compound1

Clinical Information

Launched

Isoform

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

Citation 01

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.|Harvard Medical School LINCS LIBRARY|Hong Kong Polytechnic University. 2025.|Virology. 2023 Aug:585:205-214.

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