| Size | Price | Stock | Qty |
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| Targets |
c-Met (hepatocyte growth factor receptor/HGFR) and VEGFR2 (vascular endothelial growth factor receptor 2). Canlitinib is a dual inhibitor of c-Met and VEGFR2, two key drivers of tumor growth, metastasis, and angiogenesis.
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| ln Vitro |
Canlitinib is a tyrosine kinase inhibitor that blocks both c-Met and VEGFR2 signaling. c-Met is often dysregulated in many cancers, promoting proliferation and metastasis, while VEGFR2 drives angiogenesis. By inhibiting both pathways, Canlitinib aims to suppress tumor growth both directly and by cutting off its blood supply.
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| ln Vivo |
Canlitinib is an orally bioavailable TKI. Its ability to inhibit both c-Met and VEGFR2 makes it a promising candidate for solid tumor research. By blocking these two distinct but complementary pathways, it may provide a more robust anti-tumor effect than single-target inhibitors and help overcome resistance.
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| Enzyme Assay |
Cell-free c-Met and VEGFR2 kinase assays are performed using recombinant human enzymes. The compound is incubated with the specific enzyme and a peptide substrate in the presence of ATP for 30-60 minutes. Kinase activity is measured using a luminescence-based ADP detection kit, and the half-maximal inhibitory concentration (IC50) is calculated.
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| Cell Assay |
c-Met or VEGFR2-dependent cancer cell lines are seeded in 96-well plates. After an overnight incubation, the cells are treated with increasing concentrations of Canlitinib for 72 hours. Cell viability is then assessed using the MTT assay or the CellTiter-Glo reagent. The effect on c-Met and VEGFR2 phosphorylation is measured by Western blot.
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| Animal Protocol |
For in vivo studies, Canlitinib is administered orally to mice bearing tumor xenografts. Dosing is typically once daily for 2-3 weeks. Tumor volumes are measured with calipers. At study termination, tumors are excised for pharmacodynamic analysis of c-Met and VEGFR2 target engagement and for histological analysis of microvessel density to assess anti-angiogenic effects.
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| ADME/Pharmacokinetics |
Canlitinib is an orally bioavailable small-molecule tyrosine kinase inhibitor. It is formulated for in vivo studies using vehicles such as 0.5% methylcellulose or DMSO/PEG300/Tween-80/saline mixtures. Its physicochemical properties are optimized for oral absorption, allowing for systemic exposure. Its molecular weight is 619.61 g/mol.
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| Toxicity/Toxicokinetics |
No specific toxicity data are reported for Canlitinib. As a dual c-Met/VEGFR2 inhibitor, the primary risks in a research context are on-target and may include anti-angiogenic effects on normal vasculature. The compound is for research use only and is not an approved drug for human consumption.
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| References | |
| Additional Infomation |
Kanitinib is a tyrosine kinase inhibitor that targets the oncoproteins c-Met (hepatocyte growth factor receptor; HGFR; MET) and vascular endothelial growth factor receptor 2 (VEGFR2), exhibiting potential anti-angiogenic and antitumor activity. After oral administration, Kanitinib targets and binds to c-Met and VEGFR2, thereby blocking c-Met and VEGFR2-dependent signaling pathways. This may induce death in tumor cells overexpressing c-Met and/or VEGFR2 proteins. c-Met and VEGFR2 are overexpressed in various tumor cell types and play crucial roles in tumor cell proliferation, survival, invasion, metastasis, and tumor angiogenesis.
Other information: Canlitinib (CAS 2222730-78-9) is a research compound and is not FDA-approved. It is extracted from patent WO2018072614 (IV-2). The compound is typically available as a solid (light yellow to yellow) with a purity of 97.09%. It is used as a molecular probe to study the cooperative roles of c-Met and VEGFR2 in cancer. For research use only. |
| Molecular Formula |
C33H31F2N3O7
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|---|---|
| Molecular Weight |
619.611955881119
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| Exact Mass |
619.213
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| CAS # |
2222730-78-9
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| PubChem CID |
139415233
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
6.1
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
14
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| Heavy Atom Count |
45
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| Complexity |
1010
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| Defined Atom Stereocenter Count |
0
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| SMILES |
COC1=CC2=C(C=CN=C2C=C1OCCCCCC(=O)O)OC3=C(C=C(C=C3)NC(=O)C4(CC4)C(=O)NC5=CC=C(C=C5)F)F
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| InChi Key |
PCKYITPVOLEZKL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C33H31F2N3O7/c1-43-28-18-23-25(19-29(28)44-16-4-2-3-5-30(39)40)36-15-12-26(23)45-27-11-10-22(17-24(27)35)38-32(42)33(13-14-33)31(41)37-21-8-6-20(34)7-9-21/h6-12,15,17-19H,2-5,13-14,16H2,1H3,(H,37,41)(H,38,42)(H,39,40)
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| Chemical Name |
6-[4-[2-fluoro-4-[[1-[(4-fluorophenyl)carbamoyl]cyclopropanecarbonyl]amino]phenoxy]-6-methoxyquinolin-7-yl]oxyhexanoic acid
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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 Note: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| 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) |
DMSO: 100 mg/mL (161.39 mM)
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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 | 1.6139 mL | 8.0696 mL | 16.1392 mL | |
| 5 mM | 0.3228 mL | 1.6139 mL | 3.2278 mL | |
| 10 mM | 0.1614 mL | 0.8070 mL | 1.6139 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.
Link: https://clinicaltrials.gov/ct2/show/NCT04093466
Conditions:Advanced Solid TumorLink: https://clinicaltrials.gov/ct2/show/NCT02916095
Conditions:Solid TumorsProducts are for research use only; We do not sell to patients
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