Cabozantinib hydrochloride
Based on 57 publication(s) in Google Scholar
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.
For research use only. We do not sell to patients.
- CAS No.: 1817759-42-4
- Formula: C28H25ClFN3O5
- Molecular Weight:537.97
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) Cabozantinib hydrochloride
More- Cancer Discov. 2021 Jan;11(1):126-141. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- J Clin Invest. 2026 Mar 17:e200260. [Abstract]
- MedComm (2020). 2025 Dec 8;6(12):e70492. [Abstract]
- Cell Rep Med. 2025 Apr 15;6(4):102053. [Abstract]
- Biomaterials. 2022 Oct:289:121800. [Abstract]
- Cancer Lett. 2019 Apr 10:447:105-114. [Abstract]
- J Pharm Anal. 2021 Dec;11(6):799-807. [Abstract]
- Adv Healthc Mater. 2023 Dec;12(31):e2302046. [Abstract]
- Cell Death Discov. 2026 Mar 28. [Abstract]
- Acta Pharmacol Sin. 2021 Jan;42(1):108-114. [Abstract]
- J Transl Med. 2023 Jan 9;21(1):9. [Abstract]
- Mol Med. 2025 May 27;31(1):209. [Abstract]
- Antioxidants (Basel). 2021 Aug 24;10(9):1336. [Abstract]
- Clin Transl Med. 2025 May;15(5):e70338. [Abstract]
- Br J Cancer. 2024 Aug;131(3):601-610. [Abstract]
- Br J Pharmacol. 2025 May 21. [Abstract]
- J Med Chem. 2025 Sep 25;68(18):19536-19553. [Abstract]
- J Med Chem. 2016 Jan 14;59(1):358-73. [Abstract]
- Mol Cancer Ther. 2017 Nov;16(11):2387-2398. [Abstract]
- Biochem Pharmacol. 2026 Jun:248:117843. [Abstract]
- Drug Des Devel Ther. 2018 Apr 30:12:1009-1017. [Abstract]
- Mol Cancer Res. 2019 Feb;17(2):499-507. [Abstract]
- Eur J Pharmacol. 2025 Sep 15:1003:177942. [Abstract]
- Int J Mol Sci. 2022 Sep 14;23(18):10677. [Abstract]
- Invest Ophthalmol Vis Sci. 2022 Dec 1;63(13):14. [Abstract]
- BMC Biol. 2024 Oct 1;22(1):222. [Abstract]
- Mediators Inflamm. 2020 Oct 24:2020:1649453. [Abstract]
- Sci Rep. 2019 Nov 12;9(1):16600. [Abstract]
- Cancers (Basel). 2025 Sep 9;17(18):2950. [Abstract]
- Cancers (Basel). 2024 Jan 8;16(2):269. [Abstract]
- Spectrochim Acta A Mol Biomol Spectrosc. 2016 Apr 15:159:199-208. [Abstract]
- Biomedicines. 2020 Nov 28;8(12):547. [Abstract]
- Bioengineering (Basel). 2025 Oct 19;12(10):1121. [Abstract]
- Saudi Pharm J. 2023 Oct;31(10):101756. [Abstract]
- J Neurosci. 2020 Dec 9;40(50):9602-9616. [Abstract]
- Exp Cell Res. 2020 Aug 1;393(1):112054. [Abstract]
- Front Oncol. 2022 Jul 7;12:915319. [Abstract]
- Biochem Biophys Rep. 2020 Jan 17:21:100726. [Abstract]
- J Cell Biochem. 2020 Mar;121(3):2343-2353. [Abstract]
- PLoS One. 2024 Nov 1;19(11):e0308647. [Abstract]
- PLoS One. 2017 Sep 25;12(9):e0185321. [Abstract]
- Fundam Clin Pharmacol. 2021 Oct;35(5):919-929. [Abstract]
- Virology. 2023 Aug:585:205-214. [Abstract]
- Biochem Biophys Res Commun. 2024 Nov 19:734:150781. [Abstract]
- Am J Reprod Immunol. 2021 Mar;85(3):e13352. [Abstract]
- Eur J Drug Metab Pharmacokinet. 2021 Sep;46(5):625-635. [Abstract]
- React Kinet Mech Cat. 07 January 2022.
- Biomed Chromatogr. 2024 May;38(5):e5833. [Abstract]
- Biomed Chromatogr. 2023 Sep;37(9):e5685. [Abstract]
- Biomed Chromatogr. 2020 Aug;34(8):e4862. [Abstract]
- chemRxiv. 2026 Apr 6.
- bioRxiv. 2025 May 21.
- bioRxiv. 2024 November 03.
- bioRxiv. 2023 Apr 14.
- Patent. US20220332731A1.
- Patent. US20170349880A1.
Customer Validation & Images
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All VEGFR Isoforms
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Biological Activity
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VEGFR2 0.035 ± 0. nM (IC50) |
Axl |
Flt-4 6 nM (IC50) |
Flt-1 12 nM (IC50) |
Cabozantinib hydrochloride inhibits phosphorylation of MET and VEGFR2, as well as KIT, FLT3, and AXL with IC50 values of 7.8, 1.9, 5.0, 7.5, and 42 μM, respectively[1].
Cabozantinib hydrochloride (4.6 nM) inhibits tubule formation with no evidence of cytotoxicity, with IC50 values of 6.7, 5.1, 4.1, 7.7, and 4.7 nM in HMVEC, MDA-MB-231, A431, HT1080, and B16F10 cells, respectively[1].
Cabozantinib hydrochloride (0-370 nM, 24 h) inhibits cellular migration and invasion[1].
Cabozantinib hydrochloride (48 h) inhibits tumor cell proliferation in a variety of tumor types[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SNU-5, Hs746T, SNU-1, SNU-16, MDA-MB-231, U87MG, H441, H69, and PC3 cells[1]
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Concentration:
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Incubation Time:48 hours
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Result:Inhibited tumor cell proliferation, with IC50 of 19, 9.9, 5223, 1149, 6421, 1851, 21700, 20200, and 10800 nM, respectively.
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Cell Line:B16F10 cells[1]
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Concentration:0, 41, 123, and 370 nM
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Incubation Time:24 hours
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Result:Potently inhibited HGF-induced migration (IC50 = 31 nM) of B16F10 cells.
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Cell Line:B16F10 cells[1]
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Concentration:0, 1.5, 14, and 123 nM
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Incubation Time:24 hours
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Result:Potently inhibited HGF-induced invasion (IC50 = 9 nM) of B16F10 cells.
Cabozantinib hydrochloride (100 mg/kg, Orally, once) significantly increases tumor hypoxia and apoptosis[1].
Cabozantinib hydrochloride (0-60 mg/kg, Orally, once daily for 14 days) inhibits tumor growth in a dose-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female mice bearing MBA-MB-231 tumor (5 per group)[1]
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Dosage:0, 100 mg/kg
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Administration:Orally, once
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Result:Inhibited MET and VEGFR2 phosphorylation.
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Animal Model:Mice bearing MBA-MB-231 tumor[1]
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Dosage:1, 3, 10, 30, 60 mg/kg
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Administration:Orally, once daily for 14 days
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Result:Inhibited tumor growth in a dose-dependent manner.
Chemical Information
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CAS No. 1817759-42-4
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Molecular Weight 537.97
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Formula C28H25ClFN3O5
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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
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Synonyms
XL184 hydrochloride; BMS-907351 hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (57)
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Journal Impact Factor
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Most Recent
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Cancer Discov
2021 Jan;11(1):126-141. PMID: 33004339 -
Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
J Clin Invest
Targeting Wnt/β-Catenin and circadian regulator restores PRC2/EZH2 controlled chromatin bivalency and suppresses cell state diversity. [Abstract]2026 Mar 17:e200260. PMID: 41842971 -
MedComm (2020)
Integrated Multi-Omics Profiling to Characterize Molecular Subtypes and Reveal Potential Therapeutic Strategies for Colorectal Cancer. [Abstract]2025 Dec 8;6(12):e70492. PMID: 41377767 -
Cell Rep Med
CAN-Scan: A multi-omic phenotype-driven precision oncology platform identifies prognostic biomarkers of therapy response for colorectal cancer. [Abstract]2025 Apr 15;6(4):102053. PMID: 40187357 -
Biomaterials
2022 Oct:289:121800. PMID: 36166893 -
Cancer Lett
Repurposing cabozantinib to GISTs: Overcoming multiple imatinib-resistant cKIT mutations including gatekeeper and activation loop mutants in GISTs preclinical models. [Abstract]2019 Apr 10:447:105-114. PMID: 30684595 -
J Pharm Anal
Synergistic effects of methyl 2-cyano-3,11-dioxo-18beta-olean-1,-12-dien-30-oate and erlotinib on erlotinib-resistant non-small cell lung cancer cells. [Abstract]2021 Dec;11(6):799-807. PMID: 35028186 -
Adv Healthc Mater
Dual-Targeting Nanoliposome Improves Pro-inflammatory Immunomodulation of the Tumor Microenvironment. [Abstract]2023 Dec;12(31):e2302046. PMID: 37605325 -
Cell Death Discov
CXCR4, CXCR7 and PBRM1 are responsible for everolimus and cabozantinib resistance in human renal cancer cells. [Abstract]2026 Mar 28. PMID: 41896541 -
Acta Pharmacol Sin
Osimertinib successfully combats EGFR-negative glioblastoma cells by inhibiting the MAPK pathway. [Abstract]2021 Jan;42(1):108-114. PMID: 32398685 -
J Transl Med
Papillary thyroid cancer organoids harboring BRAFV600E mutation reveal potentially beneficial effects of BRAF inhibitor-based combination therapies. [Abstract]2023 Jan 9;21(1):9. PMID: 36624452 -
Mol Med
Overexpression of c-Myc triggers p62 aggregation-mediated mitochondrial mitophagy in cabozantinib resistance of hepatocellular carcinoma. [Abstract]2025 May 27;31(1):209. PMID: 40426058 -
Antioxidants (Basel)
Antioxidants Threaten Multikinase Inhibitor Efficacy against Liver Cancer by Blocking Mitochondrial Reactive Oxygen Species. [Abstract]2021 Aug 24;10(9):1336. PMID: 34572967 -
Clin Transl Med
2025 May;15(5):e70338. PMID: 40437874 -
Br J Cancer
Zurletrectinib is a next-generation TRK inhibitor with strong intracranial activity against NTRK fusion-positive tumours with on-target resistance to first-generation agents. [Abstract]2024 Aug;131(3):601-610. PMID: 38902532 -
Br J Pharmacol
Casdatifan (AB521) is a novel and potent allosteric small molecule inhibitor of protumourigenic HIF-2α dependent transcription. [Abstract]2025 May 21. PMID: 40400177 -
J Med Chem
Discovery of APS03118, a Potent and Selective Next-Generation RET Inhibitor with a Novel Kinase Hinge Scaffold. [Abstract]2025 Sep 25;68(18):19536-19553. PMID: 40920215 -
J Med Chem
A Pyrazolo[3,4-d]pyrimidin-4-amine Derivative Containing an Isoxazole Moiety Is a Selective and Potent Inhibitor of RET Gatekeeper Mutants. [Abstract]2016 Jan 14;59(1):358-73. PMID: 26652860
Cabozantinib hydrochloride purchased from MedChemExpress. Usage Cited in: J Med Chem. 2016 Jan 14;59(1):358-73. [Abstract]
Autophosphorylation of RET and its downstream signaling are blocked by 6i. The effect of 6i on autophosphorylation of RET in (A) RET-WT Ba/F3, (B) RET-S891A Ba/F3, (C) RET-V804L Ba/F3 and (D) RET-V804M Ba/F3. (A-D) Ba/F3 cells, stably transformed with the indicated constructs, are treated for 1 h with gradually increasing concentrations of 7a, Cabozantinib and 6i (0-10 μM) and then lysed. Protein extracts are immunoblotted with antibodies specific for the Y905 and Y1062 phosphorylated forms of R
Cabozantinib hydrochloride purchased from MedChemExpress. Usage Cited in: J Med Chem. 2016 Jan 14;59(1):358-73. [Abstract]
Autophosphorylation of RET and its downstream signaling are blocked by 6i. The effect of 6i on autophosphorylation of RET in (A) RET-WT Ba/F3, (B) RET-S891A Ba/F3, (C) RET-V804L Ba/F3 and (D) RET-V804M Ba/F3. (A-D) Ba/F3 cells, stably transformed with the indicated constructs, are treated for 1 h with gradually increasing concentrations of 7a, Cabozantinib and 6i (0-10 μM) and then lysed. Protein extracts are immunoblotted with antibodies specific for the Y905 and Y1062 phosphorylated forms of R
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Mol Cancer Ther
Combination Therapy with c-Met and Src Inhibitors Induces Caspase-Dependent Apoptosis of Merlin-Deficient Schwann Cells and Suppresses Growth of Schwannoma Cells. [Abstract]2017 Nov;16(11):2387-2398. PMID: 28775147
Cabozantinib hydrochloride purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2017 Nov;16(11):2387-2398. [Abstract]
Representative Western blots and densitometry show that cabozantinib reduces phosphorylation of Erk1/2 after 6 hours and reduces cyclin D1 and increases p27 protein levels after 24 hours of treatment (n=3-4).
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Biochem Pharmacol
Cabozantinib inhibits necroptosis by targeting MLKL oligomerization and alleviates psoriasis in vivo. [Abstract]2026 Jun:248:117843. PMID: 41747872 -
Drug Des Devel Ther
Advances in the drug therapies of acute myeloid leukemia (except acute wpromyelocytic leukemia). [Abstract]2018 Apr 30:12:1009-1017. PMID: 29750014 -
Mol Cancer Res
Activation of AXL as a Preclinical Acquired Resistance Mechanism Against Osimertinib Treatment in EGFR-Mutant Non-Small Cell Lung Cancer Cells. [Abstract]2019 Feb;17(2):499-507. PMID: 30463991 -
Eur J Pharmacol
VOPP1, a determinant of the sensitivity of non-small cell lung cancer cells to NAE inhibitors. [Abstract]2025 Sep 15:1003:177942. PMID: 40651787 -
Int J Mol Sci
Chidamide plus Tyrosine Kinase Inhibitor Remodel the Tumor Immune Microenvironment and Reduce Tumor Progression When Combined with Immune Checkpoint Inhibitor in Naïve and Anti-PD-1 Resistant CT26-Bearing Mice. [Abstract]2022 Sep 14;23(18):10677. PMID: 36142591 -
Invest Ophthalmol Vis Sci
Preclinical Evaluation of Trabectedin in Combination With Targeted Inhibitors for Treatment of Metastatic Uveal Melanoma. [Abstract]2022 Dec 1;63(13):14. PMID: 36515935 -
BMC Biol
VEGF-dependent testicular vascularisation involves MEK1/2 signalling and the essential angiogenesis factors, SOX7 and SOX17. [Abstract]2024 Oct 1;22(1):222. PMID: 39354506 -
Mediators Inflamm
Activating CD137 Signaling Promotes Sprouting Angiogenesis via Increased VEGFA Secretion and the VEGFR2/Akt/eNOS Pathway. [Abstract]2020 Oct 24:2020:1649453. PMID: 33162828 -
Sci Rep
LKB1/p53/TIGAR/autophagy-dependent VEGF expression contributes to PM2.5-induced pulmonary inflammatory responses. [Abstract]2019 Nov 12;9(1):16600. PMID: 31719630 -
Cancers (Basel)
Cabozantinib Sensitizes NSCLC Cells to Radiation by Inducing Ferroptosis via STAT3/MCL1/BECN1/SLC7A11 Axis Suppression. [Abstract]2025 Sep 9;17(18):2950. PMID: 41008795 -
Cancers (Basel)
MICA+ Tumor Cell Upregulated Macrophage-Secreted MMP9 via PROS1-AXL Axis to Induce Tumor Immune Escape in Advanced Hepatocellular Carcinoma (HCC). [Abstract]2024 Jan 8;16(2):269. PMID: 38254761 -
Spectrochim Acta A Mol Biomol Spectrosc
Interaction of new kinase inhibitors cabozantinib and tofacitinib with human serum alpha-1 acid glycoprotein. A comprehensive spectroscopic and molecular Docking approach. [Abstract]2016 Apr 15:159:199-208. PMID: 26851488 -
Biomedicines
Identification of Enzymes Oxidizing the Tyrosine Kinase Inhibitor Cabozantinib: Cabozantinib Is Predominantly Oxidized by CYP3A4 and Its Oxidation Is Stimulated by cyt b5 Activity. [Abstract]2020 Nov 28;8(12):547. PMID: 33260548 -
Bioengineering (Basel)
Precision Oncology for High-Grade Gliomas: A Tumor Organoid Model for Adjuvant Treatment Selection. [Abstract]2025 Oct 19;12(10):1121. PMID: 41155119 -
Saudi Pharm J
Augmented antitumor effects of erlotinib and cabozantinib on A549 non-small cell lung cancer: In vitro and in vivo studies. [Abstract]2023 Oct;31(10):101756. PMID: 37705877 -
J Neurosci
Macrophage-Derived Vascular Endothelial Growth Factor-A Is Integral to Neuromuscular Junction Reinnervation after Nerve Injury. [Abstract]2020 Dec 9;40(50):9602-9616. PMID: 33158964 -
Exp Cell Res
Network-based analysis with primary cells reveals drug response landscape of acute myeloid leukemia. [Abstract]2020 Aug 1;393(1):112054. PMID: 32376287 -
Front Oncol
3D Ultrasound-Guided Photoacoustic Imaging to Monitor the Effects of Suboptimal Tyrosine Kinase Inhibitor Therapy in Pancreatic Tumors. [Abstract]2022 Jul 7;12:915319. PMID: 35875138 -
Biochem Biophys Rep
Cabozantinib inhibits AXL- and MET-dependent cancer cell migration induced by growth-arrest-specific 6 and hepatocyte growth factor. [Abstract]2020 Jan 17:21:100726. PMID: 32055714 -
J Cell Biochem
Vascular endothelial growth factor enhances tendon-bone healing by activating Yes-associated protein for angiogenesis induction and rotator cuff reconstruction in rats. [Abstract]2020 Mar;121(3):2343-2353. PMID: 31633245 -
PLoS One
A novel small molecule screening assay using normal human chondrocytes toward osteoarthritis drug discovery. [Abstract]2024 Nov 1;19(11):e0308647. PMID: 39485774 -
PLoS One
2017 Sep 25;12(9):e0185321. PMID: 28945796
Cabozantinib hydrochloride purchased from MedChemExpress. Usage Cited in: PLoS One. 2017 Sep 25;12(9):e0185321. [Abstract]
Treatment with Cabozantinib results in complete inhibition of the c-MET phosphorylation stimulated by HGF at nanomolar concentrations.
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Fundam Clin Pharmacol
2021 Oct;35(5):919-929. PMID: 33523504 -
Virology
Structure-based virtual screening of ROCK1 inhibitors for the discovery of Enterovirus-A71 antivirals. [Abstract]2023 Aug:585:205-214. PMID: 37384967 -
Biochem Biophys Res Commun
Cabozantinib enhances CAIX specific CAR-T cells against renal cancer by improving effector functions and augmenting tumor immune microenvironment. [Abstract]2024 Nov 19:734:150781. PMID: 39368372 -
Am J Reprod Immunol
Cytotrophoblasts suppress macrophage-mediated inflammation through a contact-dependent mechanism. [Abstract]2021 Mar;85(3):e13352. PMID: 32969101 -
Eur J Drug Metab Pharmacokinet
Differential Inhibition of Equilibrative Nucleoside Transporter 1 (ENT1) Activity by Tyrosine Kinase Inhibitors. [Abstract]2021 Sep;46(5):625-635. PMID: 34275128 -
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Biomed Chromatogr
A simple and sensitive liquid chromatography triple quadrupole mass spectrometry method for the determination of XL092 in monkey plasma and its application to pharmacokinetic study. [Abstract]2024 May;38(5):e5833. PMID: 38291606 -
Biomed Chromatogr
Preclinical pharmacokinetics and metabolism study of SCO-267, a GPR40 full agonist, in beagle dogs using ultra-high performance liquid chromatography coupled to tandem mass spectrometry. [Abstract]2023 Sep;37(9):e5685. PMID: 37189222 -
Biomed Chromatogr
LC-MS/MS assay for the quantification of foretinib in rat plasma and its application to preclinical pharmacokinetic study. [Abstract]2020 Aug;34(8):e4862. PMID: 32307722 -
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Purity & Documentation
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. [Content Brief]
[2]. You WK, et al. VEGF and c-Met blockade amplify angiogenesis inhibition in pancreatic islet cancer. Cancer Res, 2011, 71(14), 4758-4768. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Cabozantinib hydrochloride Related Classifications
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