Art. -Nr.: HY-13016

Cabozantinib

(Synonyms: XL184; BMS-907351)

58 Cited Publications

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Based on 58 publication(s) in Google Scholar

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.

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Reinheit: 99.97%
CAS. Nr.: 849217-68-1
Formel: C₂₈H₂₄FN₃O₅
Molecular Weight:501.51

Speicherung:

4°C, protect from light

* In solvent : -80°C, 2 years; -20°C, 1 year (protect from light)

Cabozantinib Chemical Structure

CAS. Nr.: 849217-68-1

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (58)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
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Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

VEGFR2

0.035 nM (IC₅₀)

Axl

Flt-4

6 nM (IC₅₀)

Flt-1

12 nM (IC₅₀)

Met

1.3 ± 1.2 nM (IC₅₀)

Alle VEGFR Isoform-spezifische Produkte anzeigen :

Alle TAM Receptor Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A498	IC₅₀	8456 nM Compound: Cabozantinib	Antiproliferative activity against human A498 cells after 48 hrs by MTT assay Antiproliferative activity against human A498 cells after 48 hrs by MTT assay	[PMID: 29057042]
A549	IC₅₀	4205 nM Compound: Cabozantinib	Growth inhibition of human A549 cells incubated for 72 hrs by CCK8 assay Growth inhibition of human A549 cells incubated for 72 hrs by CCK8 assay	[PMID: 28651979]
A549	IC₅₀	≥50 nM Compound: Cabozantinib	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay Antiproliferative activity against human A549 cells after 72 hrs by MTT assay	[PMID: 30248654]
A549	IC₅₀	9.52 μM Compound: Cabozantinib	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay Antiproliferative activity against human A549 cells after 72 hrs by MTT assay	[PMID: 30503936]
A549	IC₅₀	8.5 μM Compound: Cabozantinib	Cytotoxicity against human A549 cells assessed as reduction in cell proliferation measured after 72 hrs by MTT assay Cytotoxicity against human A549 cells assessed as reduction in cell proliferation measured after 72 hrs by MTT assay	[PMID: 30940564]
A549	IC₅₀	3.75 μM Compound: Cabozantinib	Antiproliferative activity against human A549 cells measured after 72 hrs by MTT assay Antiproliferative activity against human A549 cells measured after 72 hrs by MTT assay	[PMID: 31757525]
A549	IC₅₀	7.8 μM Compound: XL-184	Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 32738414]
A549	IC₅₀	7.21 μM Compound: Cabozantinib	Antiproliferative against human A549 cells assessed as reduction in cell viability by MTT assay Antiproliferative against human A549 cells assessed as reduction in cell viability by MTT assay	[PMID: 33045329]
A549	IC₅₀	0.76 μM Compound: 1; XL-184	Cytotoxicity against human A549 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay Cytotoxicity against human A549 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay	[PMID: 33601310]
A549	IC₅₀	15.23 μM Compound: Cabozantinib	Antiproliferation activity against human A549 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay Antiproliferation activity against human A549 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay	[PMID: 34186178]
A549	IC₅₀	0.33 μM Compound: XL-184	Antiproliferative activity against human A549 cells expressing c-Met after 48 hrs by MTT assay Antiproliferative activity against human A549 cells expressing c-Met after 48 hrs by MTT assay	[PMID: 35227978]
A549	IC₅₀	0.62 μM Compound: Cabozantinib	Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 37229832]
A549	IC₅₀	16.2 μM Compound: Cabozantinib	Antiproliferative activity against human A549 cells incubated for 3 days by MTT assay Antiproliferative activity against human A549 cells incubated for 3 days by MTT assay	[PMID: 37348260]
A549	GI₅₀	9.5 μM Compound: 4	Growth inhibition of human A549 cells Growth inhibition of human A549 cells	[PMID: 38870832]
A549/CDDP	IC₅₀	19.6 μM Compound: Cabozantinib	Antiproliferative activity against human A549/CDDP cells after 72 hrs by MTT assay Antiproliferative activity against human A549/CDDP cells after 72 hrs by MTT assay	[PMID: 30503936]
BaF3	IC₅₀	1.3 nM Compound: XL-184	Antiproliferative activity against mouse BaF3 cells harboring CD74-ROS1 G2032R mutant assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay Antiproliferative activity against mouse BaF3 cells harboring CD74-ROS1 G2032R mutant assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay	[PMID: 25733882]
BaF3	IC₅₀	1.5 nM Compound: XL-184	Antiproliferative activity against mouse BaF3 cells harboring CD74-ROS1 L2026M mutant assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay Antiproliferative activity against mouse BaF3 cells harboring CD74-ROS1 L2026M mutant assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay	[PMID: 25733882]
BaF3	IC₅₀	2.3 nM Compound: XL-184	Antiproliferative activity against mouse BaF3 cells harboring CD74-ROS1 assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay Antiproliferative activity against mouse BaF3 cells harboring CD74-ROS1 assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay	[PMID: 25733882]
BaF3	GI₅₀	0.01 μM Compound: Cabozantinib	Inhibition of TEL-fused Ret S891A mutant (unknown origin) expressed in mouse BaF3 cells assessed as cell growth inhibition after 48 hrs by MTT assay Inhibition of TEL-fused Ret S891A mutant (unknown origin) expressed in mouse BaF3 cells assessed as cell growth inhibition after 48 hrs by MTT assay	[PMID: 26652860]
BaF3	GI₅₀	0.05 μM Compound: Cabozantinib	Inhibition of wild type TEL-fused RET (unknown origin) expressed in mouse BA/F3 cells assessed as cell growth inhibition after 48 hrs by MTT assay Inhibition of wild type TEL-fused RET (unknown origin) expressed in mouse BA/F3 cells assessed as cell growth inhibition after 48 hrs by MTT assay	[PMID: 26652860]
BaF3	GI₅₀	0.89 μM Compound: Cabozantinib	Inhibition of TEL-fused Ret V804M mutant (unknown origin) expressed in mouse BA/F3 cells assessed as cell growth inhibition after 48 hrs by MTT assay Inhibition of TEL-fused Ret V804M mutant (unknown origin) expressed in mouse BA/F3 cells assessed as cell growth inhibition after 48 hrs by MTT assay	[PMID: 26652860]
BaF3	GI₅₀	0.91 μM Compound: Cabozantinib	Inhibition of TEL-fused Ret V804L mutant (unknown origin) expressed in mouse BaF3 cells assessed as cell growth inhibition after 48 hrs by MTT assay Inhibition of TEL-fused Ret V804L mutant (unknown origin) expressed in mouse BaF3 cells assessed as cell growth inhibition after 48 hrs by MTT assay	[PMID: 26652860]
BaF3	GI₅₀	3 nM Compound: Cabozantinib	Inhibition of TEL-fused VEGFR2 (unknown origin) expressed in mouse BA/F3 cells assessed as cell growth inhibition Inhibition of TEL-fused VEGFR2 (unknown origin) expressed in mouse BA/F3 cells assessed as cell growth inhibition	[PMID: 26652860]
BaF3	IC₅₀	7.5 μM Compound: XL184; BMS-907351	Inhibition of FLT3 (unknown origin) phosphorylation transfected in mouse BAF3 cells incubated for 1 to 3 hrs Inhibition of FLT3 (unknown origin) phosphorylation transfected in mouse BAF3 cells incubated for 1 to 3 hrs	[PMID: 26717201]
BaF3	IC₅₀	14 nM Compound: 2	Inhibition of KDR (unknown origin) expressed in mouse BA/F3 cells assessed as reduction in cell viability after 48 hrs by Cell titre glo-based luminescence assay Inhibition of KDR (unknown origin) expressed in mouse BA/F3 cells assessed as reduction in cell viability after 48 hrs by Cell titre glo-based luminescence assay	[PMID: 26874741]
BaF3	IC₅₀	190 nM Compound: 2	Inhibition of KIF5B/RET (unknown origin) expressed in mouse BA/F3 cells assessed as reduction in cell viability after 48 hrs by Cell titre glo-based luminescence assay Inhibition of KIF5B/RET (unknown origin) expressed in mouse BA/F3 cells assessed as reduction in cell viability after 48 hrs by Cell titre glo-based luminescence assay	[PMID: 26874741]
BaF3	IC₅₀	0.0219 μM Compound: Cabozantinib	Antiproliferative activity against mouse BA/F3 cells expressing TPR-Met after 72 hrs by CCK8 assay Antiproliferative activity against mouse BA/F3 cells expressing TPR-Met after 72 hrs by CCK8 assay	[PMID: 27068889]
BaF3	IC₅₀	889 nM Compound: Cabozantinib	Inhibition of CCDC6-RET (unknown origin) expressed in mouse BaF3 cells assessed as inhibition of cell proliferation after 72 hrs by SRB/CCK-8 assay Inhibition of CCDC6-RET (unknown origin) expressed in mouse BaF3 cells assessed as inhibition of cell proliferation after 72 hrs by SRB/CCK-8 assay	[PMID: 27131066]
BaF3	GI₅₀	>10 μM Compound: Cabozantinib	Cytotoxicity against mouse BA/F3 cells assessed as reduction in cell viability by CellTiter-Glo luminescence assay Cytotoxicity against mouse BA/F3 cells assessed as reduction in cell viability by CellTiter-Glo luminescence assay	[PMID: 27814560]
BaF3	GI₅₀	0.15 μM Compound: Cabozantinib	Growth inhibition of mouse BaF3 cells over expressing wild type RET incubated for 3 days by MTT assay Growth inhibition of mouse BaF3 cells over expressing wild type RET incubated for 3 days by MTT assay	[PMID: 29133048]
BaF3	GI₅₀	1.45 μM Compound: Cabozantinib	Growth inhibition of mouse BaF3 cells harboring RET M918T mutant incubated for 3 days by MTT assay Growth inhibition of mouse BaF3 cells harboring RET M918T mutant incubated for 3 days by MTT assay	[PMID: 29133048]
BaF3	GI₅₀	1.53 μM Compound: Cabozantinib	Growth inhibition of mouse BaF3 cells harboring RET V804L mutant incubated for 3 days by MTT assay Growth inhibition of mouse BaF3 cells harboring RET V804L mutant incubated for 3 days by MTT assay	[PMID: 29133048]
BaF3	GI₅₀	2.8 μM Compound: Cabozantinib	Growth inhibition of mouse BaF3 cells harboring RET V804M mutant incubated for 3 days by MTT assay Growth inhibition of mouse BaF3 cells harboring RET V804M mutant incubated for 3 days by MTT assay	[PMID: 29133048]
BaF3	GI₅₀	9.36 μM Compound: Cabozantinib	Growth inhibition of mouse BaF3 cells incubated for 3 days by MTT assay Growth inhibition of mouse BaF3 cells incubated for 3 days by MTT assay	[PMID: 29133048]
BaF3	IC₅₀	0.024 μM Compound: Cabozantinib	Antiproliferative activity against mouse BAF3 cells harboring TRP-MET after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BAF3 cells harboring TRP-MET after 72 hrs by CCK-8 assay	[PMID: 29146452]
BaF3	IC₅₀	0.18 μM Compound: 2	Inhibition of RET V804M mutant (unknown origin)expressed in human BaF3 cells assessed as reduction in cell viability incubated for 48 hrs by celltiter glo luminescence cell viability assay Inhibition of RET V804M mutant (unknown origin)expressed in human BaF3 cells assessed as reduction in cell viability incubated for 48 hrs by celltiter glo luminescence cell viability assay	[PMID: 32292556]
BaF3	GI₅₀	7.914 μM Compound: Cabozantinib	Cytotoxicity against mouse BaF3 cells assessed as reduction in cell proliferation measured after 48 hrs by MTS assay Cytotoxicity against mouse BaF3 cells assessed as reduction in cell proliferation measured after 48 hrs by MTS assay	[PMID: 32882611]
BaF3	IC₅₀	0.039 μM Compound: Cabozantinib	Antiprolifertive activity against mouse BaF3 cells expressing TPR-MET assessed as inhibition of cell proliferation measured after 72 hrs by Cell Titer Glo assay Antiprolifertive activity against mouse BaF3 cells expressing TPR-MET assessed as inhibition of cell proliferation measured after 72 hrs by Cell Titer Glo assay	[PMID: 35763868]
CAKI-1	IC₅₀	1.66 μM Compound: Cabozantinib	Cytotoxicity against human CAKI-1 cells assessed as reduction cell viability by MTT assay Cytotoxicity against human CAKI-1 cells assessed as reduction cell viability by MTT assay	[PMID: 34175535]
COLO 205	IC₅₀	6.6 μM Compound: Cabozantinib	Anticancer activity against human COLO 205 cells assessed as cell growth inhibition by MTT assay Anticancer activity against human COLO 205 cells assessed as cell growth inhibition by MTT assay	[PMID: 35763868]
EBC-1	IC₅₀	51.4 nM Compound: Cabozantinib	Antiproliferative activity against human EBC1 cells after 72 hrs by MTT assay Antiproliferative activity against human EBC1 cells after 72 hrs by MTT assay	[PMID: 28412159]
EBC-1	IC₅₀	4.8 nM Compound: Cabozantinib	Antiproliferative activity against human EBC1 cells after 72 hrs by MTT assay Antiproliferative activity against human EBC1 cells after 72 hrs by MTT assay	[PMID: 30248654]
EBC-1	IC₅₀	0.043 μM Compound: Cabozantinib	Anticancer activity against human EBC-1 cells assessed as cell growth inhibition by MTT assay Anticancer activity against human EBC-1 cells assessed as cell growth inhibition by MTT assay	[PMID: 35763868]
EBC-1	IC₅₀	59.2 nM Compound: Cabozantinib	Antiproliferative activity against human EBC-1 cells incubated for 3 days by MTT assay Antiproliferative activity against human EBC-1 cells incubated for 3 days by MTT assay	[PMID: 37348260]
FHC	IC₅₀	4.4 μM Compound: Cabozantinib	Cytotoxicity against human FHC cells after 72 hrs by MTT assay Cytotoxicity against human FHC cells after 72 hrs by MTT assay	[PMID: 30503936]
HBL-100	GI₅₀	17 μM Compound: 4	Growth inhibition of human HBL-100 cells Growth inhibition of human HBL-100 cells	[PMID: 38870832]
HCT-116	IC₅₀	4.67 μM Compound: XL-184	Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 32738414]
HCT-116	IC₅₀	3.78 μM Compound: Cabozantinib	Cytotoxicity against human HCT-116 cells assessed as reduction cell viability by MTT assay Cytotoxicity against human HCT-116 cells assessed as reduction cell viability by MTT assay	[PMID: 34175535]
HCT-116	IC₅₀	4 μM Compound: Cabozantinib	Cytotoxicity against human HCT-116 cells assessed as cell growth inhibition by MTT assay Cytotoxicity against human HCT-116 cells assessed as cell growth inhibition by MTT assay	[PMID: 35763868]
HEK293	IC₅₀	25.8 μM Compound: JV-985	Cytotoxicity against human HEK293 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay Cytotoxicity against human HEK293 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay	[PMID: 33214822]
HEK293	IC₅₀	0.027 μM Compound: Cabozantinib	Cytotoxicity against HEK293 cells expressing ABCG2-482-R in presence of methotrexate Cytotoxicity against HEK293 cells expressing ABCG2-482-R in presence of methotrexate	[PMID: 35944339]
HEK293	IC₅₀	0.034 μM Compound: Cabozantinib	Cytotoxicity against HEK293 cells expressing ABCG2-482-T7 in presence of methotrexate Cytotoxicity against HEK293 cells expressing ABCG2-482-T7 in presence of methotrexate	[PMID: 35944339]
HeLa	IC₅₀	>20 μM Compound: Cabozantinib	Cytotoxicity in human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity in human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31307762]
HeLa	IC₅₀	>10000 nM Compound: XL184	Antiproliferative activity against human HeLa cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay Antiproliferative activity against human HeLa cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay	[PMID: 31382120]
HeLa	IC₅₀	0.32 μM Compound: 1; XL-184	Cytotoxicity against human HeLa cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay Cytotoxicity against human HeLa cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay	[PMID: 33601310]
HeLa	IC₅₀	79.06 μM Compound: XL-184	Antiproliferative activity against human HeLa cells expressing c-Met after 48 hrs by MTT assay Antiproliferative activity against human HeLa cells expressing c-Met after 48 hrs by MTT assay	[PMID: 35227978]
HeLa	IC₅₀	1.17 μM Compound: Cabozantinib	Antiproliferative activity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 37229832]
HeLa	GI₅₀	11 μM Compound: 4	Growth inhibition of human HeLa cells Growth inhibition of human HeLa cells	[PMID: 38870832]
HepG2	IC₅₀	12 nM Compound: Cabozantinib	Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay	[PMID: 28412159]
HepG2	IC₅₀	8.3 μM Compound: JV-985	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay Cytotoxicity against human HepG2 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay	[PMID: 33214822]
HepG2	IC₅₀	3.05 μM Compound: Cabozantinib	Cytotoxicity against human HepG2 cells assessed as reduction cell viability by MTT assay Cytotoxicity against human HepG2 cells assessed as reduction cell viability by MTT assay	[PMID: 34175535]
HepG2	IC₅₀	15.58 μM Compound: Cabozantinib	Antiproliferation activity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay Antiproliferation activity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay	[PMID: 34186178]
HepG2	IC₅₀	15.01 μM Compound: Cabozantinib	Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 38086189]
HL-60	IC₅₀	22.46 μM Compound: Cabozantinib	Antiproliferative activity against human HL60 cells harboring wild type FLT3 assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human HL60 cells harboring wild type FLT3 assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 31466809]
Hs746T	IC₅₀	9.9 nM Compound: 2	Antiproliferative activity against human Hs746T cells assessed as inhibition of cell growth Antiproliferative activity against human Hs746T cells assessed as inhibition of cell growth	[PMID: 37262349]
HT-29	IC₅₀	11.5 μM Compound: Cabozantinib	Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay	[PMID: 30503936]
HT-29	IC₅₀	9.6 μM Compound: Cabozantinib	Cytotoxicity against human HT-29 cells assessed as reduction in cell proliferation measured after 72 hrs by MTT assay Cytotoxicity against human HT-29 cells assessed as reduction in cell proliferation measured after 72 hrs by MTT assay	[PMID: 30940564]
HT-29	IC₅₀	9.6 μM Compound: Cabozantinib	Cytotoxicity in human HT-29 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity in human HT-29 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31307762]
HT-29	IC₅₀	4.56 μM Compound: Cabozantinib	Antiproliferative activity against human HT-29 cells measured after 72 hrs by MTT assay Antiproliferative activity against human HT-29 cells measured after 72 hrs by MTT assay	[PMID: 31757525]
HT-29	IC₅₀	53 μM Compound: Cpd I	Antiproliferative activity against human HT-29 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human HT-29 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 32113049]
HT-29	IC₅₀	10.6 μM Compound: Cabozantinib	Anticancer activity against human HT-29 cells assessed as inhibition of cell proliferation by MTT assay Anticancer activity against human HT-29 cells assessed as inhibition of cell proliferation by MTT assay	[PMID: 32731184]
HT-29	IC₅₀	8.6 μM Compound: Cabozantinib	Cytotoxicity against human HT-29 cells assessed as cell growth inhibition by MTT assay Cytotoxicity against human HT-29 cells assessed as cell growth inhibition by MTT assay	[PMID: 35763868]
HT-29	IC₅₀	3.7 μM Compound: Cabozantinib	Antiproliferative activity against human HT-29 cells incubated for 3 days by MTT assay Antiproliferative activity against human HT-29 cells incubated for 3 days by MTT assay	[PMID: 37348260]
Huh-7	IC₅₀	4348 nM Compound: Cabozantinib	Antiproliferative activity against human HuH7 cells after 48 hrs by MTT assay Antiproliferative activity against human HuH7 cells after 48 hrs by MTT assay	[PMID: 29057042]
HUVEC	IC₅₀	7.8 μM Compound: XL184; BMS-907351	Inhibition of VEGFR-2 phosphorylation in HUVEC incubated for 1 to 3 hrs Inhibition of VEGFR-2 phosphorylation in HUVEC incubated for 1 to 3 hrs	[PMID: 26717201]
HUVEC	IC₅₀	45 nM Compound: Cabozantinib	Cytotoxicity against HUVEC after 96 hrs by MTT assay Cytotoxicity against HUVEC after 96 hrs by MTT assay	[PMID: 30248654]
HUVEC	IC₅₀	7670 nM Compound: XL184	Antiproliferative activity against HUVEC cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay Antiproliferative activity against HUVEC cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay	[PMID: 31382120]
HUVEC	IC₅₀	2.7 μg/mL Compound: Cabozantinib	Antiproliferative activity against HUVEC cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay Antiproliferative activity against HUVEC cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay	[PMID: 37453330]
K562	IC₅₀	1.9 μM Compound: Cabozantinib	Antiproliferative activity against human K562 cells incubated for 3 days by MTT assay Antiproliferative activity against human K562 cells incubated for 3 days by MTT assay	[PMID: 37348260]
L02	IC₅₀	54.97 μM Compound: 1; XL-184	Cytotoxicity against human L02 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay Cytotoxicity against human L02 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay	[PMID: 33601310]
L02	IC₅₀	>20 μM Compound: Cabozantinib	Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 38086189]
LoVo	IC₅₀	2.6 μM Compound: Cabozantinib	Anticancer activity against human LoVo cells assessed as cell growth inhibition by MTT assay Anticancer activity against human LoVo cells assessed as cell growth inhibition by MTT assay	[PMID: 35763868]
MCF7	IC₅₀	2889 nM Compound: Cabozantinib	Growth inhibition of human MCF7 cells incubated for 72 hrs by CCK8 assay Growth inhibition of human MCF7 cells incubated for 72 hrs by CCK8 assay	[PMID: 28651979]
MCF7	IC₅₀	8.57 μM Compound: Cabozantinib	Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 30503936]
MCF7	IC₅₀	5.98 μM Compound: XL-184	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 32738414]
MCF7	IC₅₀	5.4 μM Compound: Cabozantinib	Antiproliferative against human MCF-7 cells assessed as reduction in cell viability by MTT assay Antiproliferative against human MCF-7 cells assessed as reduction in cell viability by MTT assay	[PMID: 33045329]
MCF7	IC₅₀	0.45 μM Compound: 1; XL-184	Cytotoxicity against human MCF7 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay Cytotoxicity against human MCF7 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay	[PMID: 33601310]
MCF7	IC₅₀	14.26 μM Compound: Cabozantinib	Antiproliferation activity against human MCF-7 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay Antiproliferation activity against human MCF-7 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay	[PMID: 34186178]
MCF7	IC₅₀	30.87 μM Compound: XL-184	Antiproliferative activity against human MCF7 cells expressing c-Met after 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells expressing c-Met after 48 hrs by MTT assay	[PMID: 35227978]
MCF7	IC₅₀	3.15 μM Compound: Cabozantinib	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 37229832]
MCF7	IC₅₀	1.06 μM Compound: Cabozantinib	Cytotoxicity against human MCF7 cells assessed as reduction in cell viability by MTT assay Cytotoxicity against human MCF7 cells assessed as reduction in cell viability by MTT assay	[PMID: 39026631]
MDA-MB-231	IC₅₀	42 μM Compound: XL184; BMS-907351	Inhibition of KIT (unknown origin) phosphorylation transfected in human MDA-MB-231 cells incubated for 1 to 3 hrs Inhibition of KIT (unknown origin) phosphorylation transfected in human MDA-MB-231 cells incubated for 1 to 3 hrs	[PMID: 26717201]
MDA-MB-231	IC₅₀	5 μM Compound: XL184; BMS-907351	Inhibition of AXL phosphorylation in human MDA-MB-231 cells incubated for 1 to 3 hrs Inhibition of AXL phosphorylation in human MDA-MB-231 cells incubated for 1 to 3 hrs	[PMID: 26717201]
MDA-MB-231	IC₅₀	13.4 μM Compound: Cabozantinib	Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay	[PMID: 30503936]
MDA-MB-231	IC₅₀	5080 nM Compound: XL184	Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay	[PMID: 31382120]
MDA-MB-231	IC₅₀	19.72 μM Compound: Cabozantinib	Antiproliferation activity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay Antiproliferation activity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay	[PMID: 34186178]
MHCC97H	IC₅₀	25 μg/mL Compound: Cabozantinib	Antiproliferative activity against human MHCC97H cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay Antiproliferative activity against human MHCC97H cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay	[PMID: 37453330]
MHCC97H	IC₅₀	2.62 nM Compound: Cabozantinib	Antiproliferative activity against human MHCC97H cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human MHCC97H cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 38086189]
MKN-45	IC₅₀	6.9 nM Compound: Cabozantinib	Antiproliferative activity against human MKN45 cells after 72 hrs by MTT assay Antiproliferative activity against human MKN45 cells after 72 hrs by MTT assay	[PMID: 30248654]
MKN-45	IC₅₀	32 μM Compound: Cpd I	Antiproliferative activity against human MKN-45 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human MKN-45 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 32113049]
MKN-45	IC₅₀	0.14 μM Compound: Cabozantinib	Anticancer activity against human MKN-45 cells assessed as cell growth inhibition by MTT assay Anticancer activity against human MKN-45 cells assessed as cell growth inhibition by MTT assay	[PMID: 35763868]
MV4-11	IC₅₀	15.16 μM Compound: Cabozantinib	Antiproliferative activity against human MV4-11 cells harboring FLT3-ITD assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human MV4-11 cells harboring FLT3-ITD assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 31466809]
NCI-H1299	IC₅₀	1919 nM Compound: Cabozantinib	Growth inhibition of human H1299 cells incubated for 72 hrs by CCK8 assay Growth inhibition of human H1299 cells incubated for 72 hrs by CCK8 assay	[PMID: 28651979]
NCI-H1975	IC₅₀	6.67 μM Compound: Cabozantinib	Cytotoxicity in human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity in human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31307762]
NCI-H1993	IC₅₀	0.11 μM Compound: Cabozantinib	Anticancer activity against human NCI-H1993 cells assessed as cell growth inhibition by MTT assay Anticancer activity against human NCI-H1993 cells assessed as cell growth inhibition by MTT assay	[PMID: 35763868]
NCI-H292	IC₅₀	≥50 nM Compound: Cabozantinib	Antiproliferative activity against human NCI-H292 cells after 72 hrs by MTT assay Antiproliferative activity against human NCI-H292 cells after 72 hrs by MTT assay	[PMID: 30248654]
NCI-H460	IC₅₀	5669 nM Compound: Cabozantinib	Growth inhibition of human H460 cells incubated for 72 hrs by CCK8 assay Growth inhibition of human H460 cells incubated for 72 hrs by CCK8 assay	[PMID: 28651979]
NCI-H460	IC₅₀	40.1 nM Compound: Cabozantinib	Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTT assay Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTT assay	[PMID: 30248654]
NCI-H460	IC₅₀	3.6 μM Compound: Cpd I	Antiproliferative activity against human NCI-H460 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human NCI-H460 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 32113049]
NCI-H727	IC₅₀	14010 nM Compound: Cabozantinib	Antiproliferative activity against human NCI-H727 cells after 48 hrs by MTT assay Antiproliferative activity against human NCI-H727 cells after 48 hrs by MTT assay	[PMID: 29057042]
NIH3T3	GI₅₀	>10 μM Compound: Cabozantinib	Growth inhibition of human NIH3T3 cells incubated for 3 days by MTT assay Growth inhibition of human NIH3T3 cells incubated for 3 days by MTT assay	[PMID: 29133048]
NIH3T3	GI₅₀	0.1 μM Compound: Cabozantinib	Growth inhibition of human NIH3T3 cells harboring RET C634Y mutant incubated for 3 days by MTT assay Growth inhibition of human NIH3T3 cells harboring RET C634Y mutant incubated for 3 days by MTT assay	[PMID: 29133048]
PANC-1	IC₅₀	5.13 μM Compound: Cabozantinib	Cytotoxicity against human PANC-1 cells assessed as reduction cell viability by MTT assay Cytotoxicity against human PANC-1 cells assessed as reduction cell viability by MTT assay	[PMID: 34175535]
PC-3	IC₅₀	1.9 μM Compound: XL184; BMS-907351	Inhibition of c-Met phosphorylation in human PC3 cells incubated for 1 to 3 hrs Inhibition of c-Met phosphorylation in human PC3 cells incubated for 1 to 3 hrs	[PMID: 26717201]
PC-3	IC₅₀	8.25 μM Compound: Cabozantinib	Antiproliferative activity against human PC-3 cells measured after 72 hrs by MTT assay Antiproliferative activity against human PC-3 cells measured after 72 hrs by MTT assay	[PMID: 31757525]
PC-3	IC₅₀	3.68 μM Compound: Cabozantinib	Cytotoxicity against human PC-3 cells assessed as reduction cell viability by MTT assay Cytotoxicity against human PC-3 cells assessed as reduction cell viability by MTT assay	[PMID: 34175535]
PC-3	IC₅₀	2.01 μM Compound: Cabozantinib	Cytotoxicity against human PC-3 cells assessed as reduction in cell viability by MTT assay Cytotoxicity against human PC-3 cells assessed as reduction in cell viability by MTT assay	[PMID: 39026631]
Sf21	IC₅₀	16 nM Compound: 2	Inhibition of recombinant His-tagged human KDR expressed in insect Sf21 cells preincubated for 15 mins followed by substrate addition measured after 20 mins by HTRF assay Inhibition of recombinant His-tagged human KDR expressed in insect Sf21 cells preincubated for 15 mins followed by substrate addition measured after 20 mins by HTRF assay	[PMID: 26874741]
Sf21	IC₅₀	3 nM Compound: Cabozantinib	Inhibition of wild type N-terminal GST-tagged recombinant human RET (658 residues) expressed in insect Sf21 cells using poly(Glu,Tyr)4:1 as substrate incubated for 60 mins by ELISA Inhibition of wild type N-terminal GST-tagged recombinant human RET (658 residues) expressed in insect Sf21 cells using poly(Glu,Tyr)4:1 as substrate incubated for 60 mins by ELISA	[PMID: 27131066]
Sf21	IC₅₀	811 nM Compound: Cabozantinib	Inhibition of N-terminal GST-tagged recombinant human RET V804M mutant (658 residues) expressed in insect Sf21 cells using poly(Glu,Tyr)4:1 as substrate incubated for 60 mins by ELISA Inhibition of N-terminal GST-tagged recombinant human RET V804M mutant (658 residues) expressed in insect Sf21 cells using poly(Glu,Tyr)4:1 as substrate incubated for 60 mins by ELISA	[PMID: 27131066]
SiHa	IC₅₀	7940 nM Compound: XL184	Antiproliferative activity against human SiHa cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay Antiproliferative activity against human SiHa cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay	[PMID: 31382120]
SNU-5	IC₅₀	12.1 nM Compound: Cabozantinib	Antiproliferative activity against human SNU5 cells after 72 hrs by MTT assay Antiproliferative activity against human SNU5 cells after 72 hrs by MTT assay	[PMID: 30248654]
SNU-5	IC₅₀	0.056 μM Compound: Cabozantinib	Anticancer activity against human SNU-5 cells assessed as cell growth inhibition by MTT assay Anticancer activity against human SNU-5 cells assessed as cell growth inhibition by MTT assay	[PMID: 35763868]
SNU-5	IC₅₀	19 nM Compound: 2	Antiproliferative activity against human SNU-5 cells assessed as inhibition of cell growth Antiproliferative activity against human SNU-5 cells assessed as inhibition of cell growth	[PMID: 37262349]
SW1573	GI₅₀	6 μM Compound: 4	Growth inhibition of human SW1573 cells Growth inhibition of human SW1573 cells	[PMID: 38870832]
SW-620	IC₅₀	3.37 μM Compound: Cabozantinib	Cytotoxicity in human SW620 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity in human SW620 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31307762]
T47D	IC₅₀	4448 nM Compound: Cabozantinib	Growth inhibition of human T47D cells incubated for 72 hrs by CCK8 assay Growth inhibition of human T47D cells incubated for 72 hrs by CCK8 assay	[PMID: 28651979]
T47D	IC₅₀	4790 nM Compound: XL184	Antiproliferative activity against human T47D cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay Antiproliferative activity against human T47D cells assessed as reduction in cell viability measured after 72 hrs by CCK8 assay	[PMID: 31382120]
T47D	GI₅₀	16 μM Compound: 4	Growth inhibition of human T47D cells Growth inhibition of human T47D cells	[PMID: 38870832]
TT	GI₅₀	0.12 μM Compound: Cabozantinib	Inhibition of RET C634W mutant in human TT cells assessed as cell growth inhibition after 10 days by MTT assay Inhibition of RET C634W mutant in human TT cells assessed as cell growth inhibition after 10 days by MTT assay	[PMID: 26652860]
WiDr	GI₅₀	14 μM Compound: 4	Growth inhibition of human WiDr cells Growth inhibition of human WiDr cells	[PMID: 38870832]
WISH	IC₅₀	47.6 μM Compound: Cabozantinib	Cytotoxicity against human WISH cells assessed as reduction in cell viability by MTT assay Cytotoxicity against human WISH cells assessed as reduction in cell viability by MTT assay	[PMID: 39026631]

In Vitro

Cabozantinib 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 (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 (0-370 nM, 24 h) inhibits cellular migration and invasion^[1].
Cabozantinib (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.

Cell Proliferation Assay

Cell Line:

SNU-5, Hs746T, SNU-1, SNU-16, MDA-MB-231, U87MG, H441, H69, and PC3 cells^[1]
Concentration:
Incubation Time:

48 hours
Result:

Inhibited tumor cell proliferation, with IC₅₀ of 19, 9.9, 5223, 1149, 6421, 1851, 21700, 20200, and 10800 nM, respectively.

Cell Migration Assay

Cell Line:

B16F10 cells^[1]
Concentration:

0, 41, 123, and 370 nM
Incubation Time:

24 hours
Result:

Potently inhibited HGF-induced migration (IC₅₀ = 31 nM) of B16F10 cells.

Cell Invasion Assay

Cell Line:

B16F10 cells^[1]
Concentration:

0, 1.5, 14, and 123 nM
Incubation Time:

24 hours
Result:

Potently inhibited HGF-induced invasion (IC₅₀ = 9 nM) of B16F10 cells.

In Vivo

Cabozantinib (100 mg/kg, Orally, once) inhibits MET and VEGFR2 phosphorylation in mice^[1].
Cabozantinib (100 mg/kg, Orally, once) significantly increases tumor hypoxia and apoptosis^[1].
Cabozantinib (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.

Animal Model:

Female mice bearing MBA-MB-231 tumor (5 per group)^[1]
Dosage:

0, 100 mg/kg
Administration:

Orally, once
Result:

Inhibited MET and VEGFR2 phosphorylation.

Animal Model:

Mice bearing MBA-MB-231 tumor^[1]
Dosage:

1, 3, 10, 30, 60 mg/kg
Administration:

Orally, once daily for 14 days
Result:

Inhibited tumor growth in a dose-dependent manner.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 849217-68-1
Appearance Solid
Molecular Weight 501.51
Formel C₂₈H₂₄FN₃O₅
Color White to gray
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
Synonyms

XL184; BMS-907351
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, protect from light

* In solvent : -80°C, 2 years; -20°C, 1 year (protect from light)

Publications (58)

All WB

Sort by:

Journal Impact Factor

Cancer Discov

TRK xDFG Mutations Trigger a Sensitivity Switch from Type I to II Kinase Inhibitors. [Abstract]

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
Biomaterials

Automated discovery of nanomaterials via drug aggregation induced emission. [Abstract]

2022 Oct:289:121800. PMID: 36166893
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 2:102053. PMID: 40187357
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
Adv Healthc Mater

Dual-Targeting Nanoliposome Improves Pro-inflammatory Immunomodulation of the Tumor Microenvironment. [Abstract]

2023 Dec;12(31):e2302046. PMID: 37605325
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
Acta Pharmacol Sin

Osimertinib successfully combats EGFR-negative glioblastoma cells by inhibiting the MAPK pathway. [Abstract]

2021 Jan;42(1):108-114. PMID: 32398685
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 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
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
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
Clin Transl Med

Responsiveness of different MET tumour alterations to type I and type II MET inhibitors. [Abstract]

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
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 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 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
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
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
Biochem Pharmacol

Cabozantinib inhibits necroptosis by targeting MLKL oligomerization and alleviates psoriasis in vivo. [Abstract]

2026 Jun:248:117843. PMID: 41747872
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 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).
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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
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

Cabozantinib and dastinib exert anti-tumor activity in alveolar soft part sarcoma. [Abstract]

2017 Sep 25;12(9):e0185321. PMID: 28945796

Cabozantinib 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.
Fundam Clin Pharmacol

Inhibition of organic cation transporter 3 activity by tyrosine kinase inhibitors. [Abstract]

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
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
Am J Reprod Immunol

Cytotrophoblasts suppress macrophage-mediated inflammation through a contact-dependent mechanism. [Abstract]

2021 Mar;85(3):e13352. PMID: 32969101
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
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
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
React Kinet Mech Cat

07 January 2022.
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
chemRxiv

2026 Apr 6.
Hong Kong Polytechnic University

2025.
bioRxiv

2025 May 21.
bioRxiv

2024 November 03.
bioRxiv

2023 Apr 14.
Patent

US20220332731A1.
Patent

US20170349880A1.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 25 mg/mL (49.85 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.9940 mL

9.9699 mL

19.9398 mL

5 mM

0.3988 mL

1.9940 mL

3.9880 mL

10 mM

0.1994 mL

0.9970 mL

1.9940 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (protect from light). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (4.98 mM); Clear solution

Protocol 2

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (4.15 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 3

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 0.5 mg/mL (1.00 mM); Clear solution

This protocol yields a clear solution of ≥ 0.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 4

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 0.5 mg/mL (1.00 mM); Clear solution

This protocol yields a clear solution of ≥ 0.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 0.5% CMC/saline water

Solubility: 2.5 mg/mL (4.98 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
SDS (393 KB)
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COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.9940 mL	9.9699 mL	19.9398 mL	49.8495 mL
	5 mM	0.3988 mL	1.9940 mL	3.9880 mL	9.9699 mL
	10 mM	0.1994 mL	0.9970 mL	1.9940 mL	4.9849 mL
	15 mM	0.1329 mL	0.6647 mL	1.3293 mL	3.3233 mL
	20 mM	0.0997 mL	0.4985 mL	0.9970 mL	2.4925 mL
	25 mM	0.0798 mL	0.3988 mL	0.7976 mL	1.9940 mL
	30 mM	0.0665 mL	0.3323 mL	0.6647 mL	1.6616 mL
	40 mM	0.0498 mL	0.2492 mL	0.4985 mL	1.2462 mL

Cabozantinib

58 Cited Publications

100 mg Angebot einholen

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Cabozantinib

Apoptosis Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

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Publications Citing Use of MedChemExpress (MCE) Cabozantinib

Alle VEGFR Isoform-spezifische Produkte anzeigen

Alle TAM Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (58)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Cabozantinib Related Classifications

HY-13016 Related Classifications