| Size | Price | Stock | Qty |
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| 10mg |
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| 500mg |
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| Other Sizes |
| Targets |
Cabozantinib HCl targets multiple receptor tyrosine kinases (RTKs), including VEGFR2, MET, KIT, RET, AXL, and TIE2. By inhibiting these kinases, it blocks key signaling pathways involved in tumor angiogenesis, proliferation, and metastasis. Its potent inhibition of VEGFR2 (IC50 = 0.035 nM) is particularly important for its anti-angiogenic effects, while inhibition of MET (IC50 = 1.3 nM) contributes to its anti-tumor activity.
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| ln Vitro |
Cabozantinib hydrochloride, with IC50 values of 7.8, 1.9, 5.0, 7.5, and 42 μM, respectively, suppresses the phosphorylation of MET and VEGFR2, as well as KIT, FLT3, and AXL [1]. In HMVEC, MDA-MB-231, A431, HT1080, and B16F10 cells, respectively, capozantinib hydrochloride (4.6 nM) suppresses renal tubule development without exhibiting any signs of cytotoxicity. both 4.7 and 7.7 nM[1]. Inhibiting cell migration and invasion, cabotezantinib hydrochloride (0-370 nM, 24 hours) is used [1]. Inhibiting the growth of tumor cells in different types of tumors is possible with cabotinib hydrochloride (48 hours) [1].
In vitro, Cabozantinib HCl inhibits tumor cell proliferation in a variety of tumor types. It is a potent inhibitor of multiple RTKs, with IC50 values of 0.035 nM for VEGFR2, 1.3 nM for MET, 4.6 nM for KIT, 5.2 nM for RET, and 7 nM for AXL. These values demonstrate its high potency against these kinase targets. |
| ln Vivo |
Cabozantinib hydrochloride (100 mg/kg, orally, once) suppresses MET and VEGFR2 phosphorylation in mice [1]. Cabozantinib hydrochloride (100 mg/kg, orally, once) dramatically enhances tumor hypoxia and apoptosis [1]. Cabozantinib hydrochloride (0-60 mg/kg, orally, once daily for 14 days) suppresses tumor development in a dose-dependent manner [1].
In vivo, Cabozantinib HCl has been shown to inhibit tumor growth in a dose-dependent manner. In animal models, oral administration at doses of 0-60 mg/kg once daily for 14 days resulted in dose-dependent tumor growth inhibition. This confirms its in vivo efficacy as an anticancer agent. |
| Enzyme Assay |
Cabozantinib HCl is a potent inhibitor of multiple receptor tyrosine kinases. Cell-free assays typically involve measuring the inhibition of kinase activity using recombinant enzymes and peptide substrates. The compound's IC50 values for various kinases, such as 0.035 nM for VEGFR2 and 1.3 nM for MET, are determined in such assays. These assays confirm its direct inhibition of the target kinases.
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| Cell Assay |
Cell Proliferation Assay
Cell Types: SNU-5, Hs746T, SNU-1, SNU-16, MDA-MB-231, U87MG, H441, H69 and PC3 cells [1] Tested Concentrations: Incubation Duration: 48 hrs (hours) Experimental Results: Inhibition of tumor cell proliferation , IC50 are 19, 9.9, 5223, 1149, 6421, 1851, 21700, 20200 and 10800 nM respectively. Cell migration assay Cell Types: B16F10 cells [1] Tested Concentrations: 0, 41, 123 and 370 nM Incubation Duration: 24 hrs (hours) Experimental Results: Effectively inhibited HGF-induced B16F10 cell migration (IC50 = 31 nM). Cell invasion assay Cell Types: B16F10 cells [1] Tested Concentrations: 0, 1.5, 14 and 123 nM Incubation Duration: 24 hrs (hours) Experimental Results: Effectively inhibited HGF-induced B16F10 cell invasion (IC50 = 9 nM). Cellular assays for Cabozantinib HCl typically involve assessing its effects on tumor cell proliferation and signaling pathways. Cells are treated with the compound, and cell viability is measured. The compound's ability to inhibit downstream signaling, such as phosphorylation of MET and VEGFR2, can be assessed by Western blotting. Specific protocols are not detailed. |
| Animal Protocol |
Animal/Disease Models: Female mice bearing MBA-MB-231 tumors (5 per group) [1]
Doses: 0, 100 mg/kg Route of Administration: Orally, once Experimental Results:Inhibition of MET and VEGFR2 phosphorylation. Animal/Disease Models: MBA-MB-231 tumor-bearing mice [1] Doses: 1, 3, 10, 30, 60 mg/kg Route of Administration: Orally, one time/day for 14 days Experimental Results: Inhibited in a dose-dependent manner Tumor growth. In vivo animal experiments with Cabozantinib HCl have been conducted in tumor xenograft models. In one study, the compound was administered orally at doses of 0-60 mg/kg once daily for 14 days. Tumor growth was measured, and the compound inhibited tumor growth in a dose-dependent manner. These studies demonstrate its in vivo antitumor activity. |
| ADME/Pharmacokinetics |
Cabozantinib HCl is an orally bioavailable compound. Specific pharmacokinetic parameters, such as half-life, Cmax, and AUC, are not provided in the available sources. The compound is typically administered orally once daily in clinical settings. Its pharmacokinetic profile supports its use as an oral anticancer therapy.
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| Toxicity/Toxicokinetics |
Toxicity data for Cabozantinib HCl are not detailed in the available sources. As an FDA-approved drug, its safety profile is well established. Common adverse effects include hypertension, fatigue, diarrhea, and hand-foot skin reaction. Specific toxicological information is not provided in the references cited.
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| References | |
| Additional Infomation |
Cabozantinib HCl (CAS: 1817759-42-4) is a potent, orally active multi-tyrosine kinase inhibitor. It is also known as XL184 hydrochloride and is marketed under the brand names Cometriq and Cabometyx. It inhibits VEGFR2 (IC50 = 0.035 nM), MET (IC50 = 1.3 nM), KIT (IC50 = 4.6 nM), RET (IC50 = 5.2 nM), and AXL (IC50 = 7 nM). It is indicated for the treatment of advanced renal cell carcinoma, hepatocellular carcinoma, and medullary thyroid cancer.
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| Molecular Formula |
C28H25CLFN3O5
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|---|---|
| Molecular Weight |
537.966609716415
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| Exact Mass |
537.146
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| CAS # |
1817759-42-4
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| Related CAS # |
Cabozantinib;849217-68-1
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| PubChem CID |
122573030
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| Appearance |
Typically exists as solid at room temperature
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
38
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| Complexity |
795
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C(C1(CC1)C(=O)NC1C=CC(F)=CC=1)(=O)NC1C=CC(OC2=CC=NC3C=C(OC)C(OC)=CC2=3)=CC=1.Cl
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| InChi Key |
LCNVAOXPKXBXEH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C28H24FN3O5.ClH/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);1H
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| Chemical Name |
1-N-[4-(6,7-dimethoxyquinolin-4-yl)oxyphenyl]-1-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide;hydrochloride
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8588 mL | 9.2942 mL | 18.5884 mL | |
| 5 mM | 0.3718 mL | 1.8588 mL | 3.7177 mL | |
| 10 mM | 0.1859 mL | 0.9294 mL | 1.8588 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.
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