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10mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Purity: ≥98%
Cabozantinib (formerly known as XL-184 or BMS-907351; trade name Cometriq) is a novel, orally bioavailable and potent VEGFR2 inhibitor with anticancer activity. Its IC50 of 0.035 nM is sufficient to inhibit VEGFR2. This inhibitor of multiple receptor tyrosine kinase (RTK) also inhibits c-Met, Ret, Kit, Flt-1/3/4, Tie2, and AXL, with IC50 values in cell-free assays of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM, and 7 nM, respectively. A number of tyrosine receptor kinases are strongly bound by capozantinib and inhibited by it. The FDA in the United States approved cabotezantinib in November 2012 to treat medullary thyroid cancer.
Targets |
VEGFR2 (IC50 = 0.035 nM); Flt-4 (IC50 = 6 nM); Flt-1 (IC50 = 12 nM); Met (IC50 = 1.3 ± 1.2 nM)
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ln Vitro |
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ln Vivo |
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Enzyme Assay |
In addition to inhibiting c-Met, Ret, Kit, Flt-1/3/4, Tie2, and AXL with IC50 values of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM, and 7 nM, respectively, cabotinib (XL184, BMS-907351) is a potent inhibitor of VEGFR2.
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Cell Assay |
For 48 hours, different XL184 concentrations are applied to the cells. Using the CellTiter96 Aqueous Non-Radioactive Cell Proliferation Assay kit, MTS assays are used to measure cell growth. The wavelength at which absorbance is measured is 490 nm, and the treated cells' absorbance values are expressed as a percentage of the untreated cells' absorbance.
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Animal Protocol |
RIP-Tag2 transgenic mice in a C57BL/6 background with spontaneous pancreatic islet tumors
~60 mg/kg Oral gavage |
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References |
Molecular Formula |
C28H24FN3O5
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Molecular Weight |
501.51
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Exact Mass |
501.17
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Elemental Analysis |
C, 67.06; H, 4.82; F, 3.79; N, 8.38; O, 15.95
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CAS # |
849217-68-1
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Related CAS # |
Cabozantinib S-malate;1140909-48-3;Cabozantinib-d6;1802168-46-2;Cabozantinib hydrochloride;1817759-42-4;Cabozantinib-d4;1802168-53-1
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Appearance |
white solid powder
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SMILES |
COC1=CC2=C(C=CN=C2C=C1OC)OC3=CC=C(C=C3)NC(=O)C4(CC4)C(=O)NC5=CC=C(C=C5)F
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InChi Key |
ONIQOQHATWINJY-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C28H24FN3O5/c1-35-24-15-21-22(16-25(24)36-2)30-14-11-23(21)37-20-9-7-19(8-10-20)32-27(34)28(12-13-28)26(33)31-18-5-3-17(29)4-6-18/h3-11,14-16H,12-13H2,1-2H3,(H,31,33)(H,32,34)
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Chemical Name |
1-N-[4-(6,7-dimethoxyquinolin-4-yl)oxyphenyl]-1-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
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Synonyms |
Cabozantinib; XL-184; BMS-907351; BMS907351; XL184; XL 184; BMS 907351; Cabozantinib free base; trade name Cometriq
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.98 mM) (saturation unknown) in 5% DMSO + 95% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.15 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. View More
Solubility in Formulation 3: 2.08 mg/mL (4.15 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Solubility in Formulation 4: ≥ 2.08 mg/mL (4.15 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL corn oil and mix evenly. Solubility in Formulation 5: 2% DMSO +30%PEG 300 +5% Tween 80 +ddH2O: 2mg/mL Solubility in Formulation 6: 2.5 mg/mL (4.98 mM) in 0.5% CMC/saline water (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. |
Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT04804813 | Active Recruiting |
Drug: Cabozantinib | Renal Cell Carcinoma | Takeda | March 29, 2021 | |
NCT04868773 | Active Recruiting |
Drug: Cabozantinib Drug: TAS-102 |
CRC Metastatic Cancer |
University of California, Irvine | July 16, 2021 | Phase 1 |
NCT04416646 | Active Recruiting |
Drug: Cabozantinib | Renal Cell Carcinoma | Istituto Oncologico Veneto IRCCS | February 27, 2019 | |
NCT04400474 | Active Recruiting |
Drug: Cabozantinib 40 mg | Adenocarcinoma Paraganglioma |
Grupo Espanol de Tumores Neuroendocrinos |
October 7, 2020 | Phase 2 |
NCT05200143 | Active Recruiting |
Drug: Ipilimumab Drug: Cabozantinib |
Refractory Cutaneous Melanoma | Providence Health & Services | June 8, 2022 | Phase 2 |
td> |
The multi-tyrosine kinase inhibitor, XL184, targeting MET and VEGFR2 abrogates MPNST migration, invasion, and angiogenesis. Clin Cancer Res. 2011 Jun 15;17(12):3943-55. td> |
XL184 abrogates local and metastatic MPNST growth in vivo. Clin Cancer Res. 2011 Jun 15;17(12):3943-55. td> |