Cabozantinib (Synonyms: XL184; BMS-907351)

Name: Cabozantinib
Brand: MedChemExpress
SKU: HY-13016
Rating: 5.0 (45 reviews)

Cat. No.: HY-13016 Purity: 99.96%: FAQs
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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.

For research use only. We do not sell to patients.

Cabozantinib Chemical Structure

CAS No. : 849217-68-1

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 55	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 55	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 50	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 70	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 90	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 120	In-stock	Estimated Time of Arrival: December 31
200 mg	USD 190	In-stock	Estimated Time of Arrival: December 31
500 mg	USD 380	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 45 publication(s) in Google Scholar

Other Forms of Cabozantinib:

41 Publications Citing Use of MCE Cabozantinib

: 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).

: 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.

: 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

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Axl Mer Tyro3

Biological Activity
Purity & Documentation
References
Customer Review

Description

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)

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	≥ 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	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	0.76 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	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	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	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	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	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	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/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	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	0.01 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	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	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	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	0.15 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	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	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	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	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	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	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	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	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	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]
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]
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	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]
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]
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	4.67 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]
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]
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	> 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	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]
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	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	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	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]
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]
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	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	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	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	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]
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	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	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	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]
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]
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	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	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	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	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	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]
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	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]
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	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]
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	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]
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-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	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-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	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-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	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	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]
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]
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]
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]

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

Molecular Weight

501.51

Formula

C₂₈H₂₄FN₃O₅

CAS No.

849217-68-1

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the Complete Stock Solution Preparation Table

* 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.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 3

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.08 mg/mL (4.15 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 4

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (4.15 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.96%

Select Batch:

Data Sheet (282 KB) SDS (393 KB)

COA (251 KB) LCMS (110 KB)

Handling Instructions (2659 KB)

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]

[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]

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 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Cabozantinib (Synonyms: XL184; BMS-907351)

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Cabozantinib (Synonyms: XL184; BMS-907351)

Customer Review

Other Forms of Cabozantinib:

Cabozantinib Related Antibodies

41 Publications Citing Use of MCE Cabozantinib

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All VEGFR Isoform Specific Products:

View All TAM Receptor Isoform Specific Products:

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Complete Stock Solution Preparation Table

Cabozantinib Related Classifications

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