Cabozantinib malate (XL184)
Catalog No.S4001
Molecular Weight(MW): 635.59
Cabozantinib malate (XL184) is the malate of Cabozantinib, a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret, Kit, Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM in cell-free assays, respectively.
7 Customer Reviews
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Effects of AXL inhibitors on induction of pAKT and rescue of pERK following AXL overexpression. R428, 500 nmol/L; XL184, 3 umol/L; XL880, 100 nmol/L; in the presence or absence of 2 umol/L PLX4720. shAXL is a positive control.
Cancer Discov 2014 4(7), 816-27. Cabozantinib malate (XL184) purchased from Selleck.
Immunoblots of whole cell lysates from (A) LC2/ad NSCLC cells treated with BLU-667, cabozantinib, or vandetanib at indicated concentrations (nM) for 90 minutes. Phospho- and total RET, SHC, and ERK1/2 were interrogated. In LC2/ad cells, P-ERK is represented by the top two bands of the triplet.
Cancer Discov, 2018, doi:10.1158/2159-8290.CD-18-0338. Cabozantinib malate (XL184) purchased from Selleck.
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Cabozantinib reduces viability and spheroid and colony formation of GCTB stromal cells. (a) Adherent-growing GCTB stromal cells derived from three different patients were left untreated (CO) or were treated with cabozantinib (10 uM, XL184) or methotrexate (100 uM, MTX). Seventy-two hours later, the viability was measured by the MTT assay, and the control was set to 100%. (b) Spheroidal cultures were established as described in b. After spheroid formation, the cells were left untreated or were treated as described above. Seven days later, spheroids were photographed, and the number and volume of spheroids (spheroid surface) were determined. The data shown are the mean盨.D. (*P<0.05; **P<0.01).
Cell Death Dis 2014 5, e1471. Cabozantinib malate (XL184) purchased from Selleck.
Cell Death Dis 2013 4, e627. Cabozantinib malate (XL184) purchased from Selleck.
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The effect of cabozantinib on the accumulation of Dox and Rho123. (A) Fluorescence microscopy observation of the accumulation of Dox and Rho123. The scale bars represent 100 uM. (B) The accumulation of Dox and Rho123 was measured by flow cytometric analysis. The data were analysed using Kaluza software and are presented as fold-change in fluorescence intensity relative to the control HepG2/adr cells. The results are shown as the mean ± SD of three independent trials. *P < 0.05 vs. the control group.
Liver Int 2014 10.1111/liv.12524. Cabozantinib malate (XL184) purchased from Selleck.
A summary of the postcabozantinib (Cabo.) changes in bone-seeking radionuclide uptake at sites of remodeling bone. C, A line graph of the SUV mean for 99m Tc-MDP uptake at the site of the fracture in the tibia shows the impact of cabozantinib therapy on radionuclide accumulation. Animals were treated once daily with cabozantinib at 30 mg/kg 1 day after the first SPECT scan. D, Representative maximum-intensity projection (MIP) images whose intensities were manually gated to provide a clear view of radionuclide uptake at the fracture site and the nearby anatomy. Quantification was not conducted using the MIP images; the MIP images are merely provided to show a global view of 99mTc-MDP distribution in the skeleton while underscoring the foci of high radionuclide uptake at the fracture. Unfortunately, centering the images on the slices with the fracture excluded the rest of the anatomy, resulting in images that are difficult to interpret visually. *p< .01. Rx 5 treatment.
Mol Imaging 2014 10.2310/7290.2014.00026. Cabozantinib malate (XL184) purchased from Selleck.
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Inhibition of breast cancer cell growth using XL184. MCF-7 breast cancer cells were treated with increasing concentrations of XL-184 for 5 days. Cell number was measured using a colorimetric growth assay (crystal violet stain) and expressed relative to DMSO treated control cells.
Christina W Yde/CDM Danish Cancer Society Research Center Denmark. Cabozantinib malate (XL184) purchased from Selleck.
Purity & Quality Control
Choose Selective VEGFR Inhibitors
Biological Activity
| Description | Cabozantinib malate (XL184) is the malate of Cabozantinib, a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret, Kit, Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM in cell-free assays, respectively. | ||||
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| Targets |
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| In vitro |
Cabozantinib has weak inhibitory activity against RON and PDGFRβ with IC50 of 124 nM and 234 nM, respectivey, and has low activity against FGFR1 with IC50 of 5.294 μM. [1] Cabozantinib at low concentration (0.1-0.5 μM) is sufficient to induce marked inhibition of constitutive and inducible Met phosphorylation and its resultant downstream signaling in MPNST cells, and inhibit HGF-induced MPNST cell migration and invasion. Cabozantinib also induces marked inhibition of Met and VEGFR2 phosphorylation in cytokine-stimulated human umbilical vein endothelial cells (HUVECs). Although Cabozantinib has no significant effect on MPNST cell growth at 0.1 μM, Cabozantinib at 5-10 μM significantly inhibits the MPNST cell growth. [2] |
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| In vivo | Cabozantinib treatment at 30 mg/kg in RIP-Tag2 mice with spontaneous pancreatic islet tumors disrupts 83% of the tumor vasculature, reduces pericytes and empty basement membrane sleeves, causes widespread intratumoral hypoxia and extensive tumor cell apoptosis, and slows regrowth of the tumor vasculature after drug withdrawal, more significantly compared with XL999 that blocks VEGFR but not c-Met, leading to only 43% reduction in vascularity, suggesting that concurrent inhibition of VEGFR and other functionally relevant receptor tyrosine kinases (RTK) amplifies angiogenesis inhibition. Cabozantinib also decreases invasiveness of primary tumors and reduces metastasis. [1] Cabozantinib at 30 mg/kg/day significantly abrogates human MPNST xenografts growth and metastasis in SCID mice. [2] Administration of Cabozantinib induces dose-dependent inhibition of tumor growth in breast, lung, and glioma tumor models, in association with decreased tumor and endothelial cell proliferation as well as increased apoptosis. A single oral dose of Cabozantinib is sufficient to induce sustained tumor growth inhibition in MDA-MB-231 tumor-bearing mice and C6 tumor-bearing rats at 100 mg/kg and 10 mg/kg, respectively. [3] |
Protocol
| Cell Research: [2]
Cells are exposed to various concentrations of Cabozantinib for 48 hours. Cell growth is determined by MTS assays using CellTiter96 Aqueous Non-Radioactive Cell Proliferation Assay kit. Absorbance is measured at a wavelength of 490 nm, and the absorbance values of treated cells are presented as a percentage of the absorbance of untreated cells. | |
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| Animal Research: [1]
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Solubility (25°C)
| In vitro | DMSO | 100 mg/mL (157.33 mM) |
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| Water | Insoluble | |
| Ethanol | Insoluble | |
| In vivo | Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 30% propylene glycol, 5% Tween 80, 65% D5W For best results, use promptly after mixing. |
15 mg/mL |
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Information
| Molecular Weight | 635.59 |
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| Formula | C28H24FN3O5.C4H6O5 |
| CAS No. | 1140909-48-3 |
| Storage | powder |
| in solvent | |
| Synonyms | N/A |
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Clinical Trial Information
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT03586973 | Recruiting | Advanced Hepatocellular Carcinoma | Takeda | July 9 2018 | Phase 2 |
| NCT02496208 | Recruiting | Bladder Small Cell Neuroendocrine Carcinoma|Clear Cell Renal Cell Carcinoma|Infiltrating Bladder Urothelial Carcinoma Sarcomatoid Variant|Infiltrating Bladder Urothelial Carcinoma Plasmacytoid Variant|Kidney Medullary Carcinoma|Metastatic Malignant Neoplasm in the Bone|Metastatic Penile Carcinoma|Metastatic Renal Cell Carcinoma|Renal Pelvis Urothelial Carcinoma|Sarcomatoid Renal Cell Carcinoma|Squamous Cell Carcinoma of the Penis|Stage III Bladder Adenocarcinoma AJCC v6 and v7|Stage III Bladder Squamous Cell Carcinoma AJCC v6 and v7|Stage III Bladder Urothelial Carcinoma AJCC v6 and v7|Stage III Penile Cancer AJCC v7|Stage III Renal Cell Cancer AJCC v7|Stage III Renal Pelvis Cancer AJCC v7|Stage III Ureter Cancer AJCC v7|Stage III Urethral Cancer AJCC v7|Stage IIIa Penile Cancer AJCC v7|Stage IIIb Penile Cancer AJCC v7|Stage IV Bladder Adenocarcinoma AJCC v7|Stage IV Bladder Squamous Cell Carcinoma AJCC v7|Stage IV Bladder Urothelial Carcinoma AJCC v7|Stage IV Penile Cancer AJCC v7|Stage IV Renal Cell Cancer AJCC v7|Stage IV Renal Pelvis Cancer AJCC v7|Stage IV Ureter Cancer AJCC v7|Stage IV Urethral Cancer AJCC v7|Ureter Urothelial Carcinoma|Urethral Urothelial Carcinoma | National Cancer Institute (NCI) | July 9 2015 | Phase 1 |
| NCT02867592 | Recruiting | Adrenal Cortex Carcinoma|Alveolar Soft Part Sarcoma|Central Nervous System Neoplasm|Childhood Clear Cell Sarcoma of Soft Parts|Clear Cell Sarcoma of Soft Tissue|Ewing Sarcoma|Hepatoblastoma|Hepatocellular Carcinoma|MITF Positive|Osteosarcoma|Recurrent Adrenal Cortex Carcinoma|Recurrent Alveolar Soft Part Sarcoma|Recurrent Ewing Sarcoma|Recurrent Hepatoblastoma|Recurrent Hepatocellular Carcinoma|Recurrent Malignant Central Nervous System Neoplasm|Recurrent Malignant Solid Neoplasm|Recurrent Osteosarcoma|Recurrent Renal Cell Carcinoma|Recurrent Rhabdomyosarcoma|Recurrent Soft Tissue Sarcoma|Recurrent Soft Tissue Sarcoma Excluding Rhabdomyosarcoma|Recurrent Thyroid Gland Medullary Carcinoma|Refractory Ewing Sarcoma|Refractory Malignant Central Nervous System Neoplasm|Refractory Malignant Solid Neoplasm|Refractory Osteosarcoma|Refractory Rhabdomyosarcoma|Refractory Soft Tissue Sarcoma|Refractory Soft Tissue Sarcoma Excluding Rhabdomyosarcoma|Renal Cell Carcinoma|Rhabdomyosarcoma|Soft Tissue Sarcoma Excluding Rhabdomyosarcoma|Solid Neoplasm|Thyroid Gland Medullary Carcinoma|Wilms Tumor | National Cancer Institute (NCI) | May 8 2017 | Phase 2 |
| NCT01630590 | Active not recruiting | Prostate Cancer | M.D. Anderson Cancer Center|Exelixis|High Impact Clinical Research Support Program | January 8 2014 | Phase 2 |
| NCT01835158 | Active not recruiting | Clear Cell Renal Cell Carcinoma|Metastatic Renal Cell Cancer|Stage III Renal Cell Cancer AJCC v7|Stage IV Renal Cell Cancer AJCC v7 | National Cancer Institute (NCI) | July 8 2013 | Phase 2 |
| NCT01811212 | Completed | Poorly Differentiated Thyroid Gland Carcinoma|Recurrent Thyroid Gland Carcinoma|Stage I Thyroid Gland Follicular Carcinoma|Stage I Thyroid Gland Papillary Carcinoma|Stage II Thyroid Gland Follicular Carcinoma|Stage II Thyroid Gland Papillary Carcinoma|Stage III Thyroid Gland Follicular Carcinoma|Stage III Thyroid Gland Papillary Carcinoma|Stage IVA Thyroid Gland Follicular Carcinoma|Stage IVA Thyroid Gland Papillary Carcinoma|Stage IVB Thyroid Gland Follicular Carcinoma|Stage IVB Thyroid Gland Papillary Carcinoma|Stage IVC Thyroid Gland Follicular Carcinoma|Stage IVC Thyroid Gland Papillary Carcinoma|Tall Cell Variant Thyroid Gland Papillary Carcinoma|Thyroid Gland Oncocytic Follicular Carcinoma | National Cancer Institute (NCI)|Exelixis | May 8 2013 | Phase 2 |
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