| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Targets |
CT-053 tosylate targets multiple tyrosine kinases including c-Met, VEGFR2, Axl, and potentially other kinases. It acts as a potent inhibitor of these kinases. By inhibiting VEGFR2, it blocks angiogenesis. By inhibiting c-Met and Axl, it modulates tumor growth and metastasis.
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| ln Vitro |
Ningetinib Tosylate is a strong, orally accessible, small molecule tyrosine kinase inhibitor (TKI) with IC50 values of 6.7, 1.9, and <1.0 nM for c-Met, VEGFR2, and Axl, respectively. In cell-based functional studies, Ningetinib Tosylate (CT053PTSA) reduced HGF- and VEGF-stimulated HUVEC proliferation and microangiogenesis in rat aortic rings with IC50 values of 8.6 and 6.3 nM, respectively [1].
CT-053 tosylate inhibits c-Met, VEGFR2, and Axl with IC50 values of 6.7 nM, 1.9 nM, and <1.0 nM, respectively. In cell-based functional studies, it effectively inhibits the phosphorylation of these kinases. It is a potent VEGF and PDGF inhibitor. |
| ln Vivo |
Ningetinib Tosylate (CT053PTSA) efficiently reduced the phosphorylation of c-Met and its downstream signaling kinases AKT and ERK1/2 in tumor tissues for up to 6 hours when given as a single oral dose (3 mg/kg) to U87MG tumor-bearing nude mice. Oral ninggotinib tosylate at a dose of 20 mg/kg/day increased lifetime value (ILS= 32%, p=0.003) and lengthened the median survival time (MST) in the orthotopic U87MG human glioblastoma xenograft model. 21 days) in contrast to the group receiving vehicle therapy [1].
CT-053 tosylate efficiently reduced the phosphorylation of c-Met and its downstream signaling kinases AKT and ERK1/2 in tumor tissues for up to 6 hours when given as a single oral dose (3 mg/kg) to U87MG tumor-bearing nude mice. It has potential for the treatment of wet age-related macular degeneration. |
| Enzyme Assay |
CT-053 tosylate is evaluated in cell-free kinase assays using purified c-Met, VEGFR2, and Axl enzymes. The compound is incubated with the kinase, ATP, and a substrate, and the inhibition of kinase activity is measured. IC50 values are determined to quantify the potency of inhibition.
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| Cell Assay |
CT-053 tosylate is assessed in cell-based assays using cancer cell lines. Cells are treated with CT-053 tosylate, and the phosphorylation of c-Met, VEGFR2, and Axl is measured by Western blot analysis. Cell proliferation and survival are evaluated.
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| Animal Protocol |
CT-053 tosylate is administered orally in animal models to evaluate its antitumor efficacy. In U87MG tumor-bearing nude mice, a single oral dose of 3 mg/kg efficiently reduced the phosphorylation of c-Met and its downstream signaling kinases AKT and ERK1/2 for up to 6 hours.
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| ADME/Pharmacokinetics |
CT-053 tosylate has a molecular weight of 571.65 and a molecular formula of C31H31FN4O4S. It has a CAS number of 1394820-77-9. The compound is soluble in DMSO. It should be stored under recommended conditions.
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| Toxicity/Toxicokinetics |
No detailed toxicity data is available for CT-053 tosylate. The compound is for research use only and is not intended for human therapeutic use. It is a potent tyrosine kinase inhibitor.
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| References | |
| Additional Infomation |
Ningetinib tosylate is the tosylate form of Ningetinib, an orally potent receptor tyrosine kinase inhibitor that inhibits c-MET/hepatocyte growth factor receptor (HGFR), vascular endothelial growth factor receptor 2 (VEGFR2 KDR), Axl (UFO), Mer, and Fms-like tyrosine kinase 3 (Flt3; CD135; STK1; FLK2), exhibiting antitumor activity. Upon administration, Ningetinib binds to multiple kinases, including c-Met, VEGFR2, Axl, Mer, and Flt3, thereby inhibiting their signaling pathways. This inhibits the growth, angiogenesis, and metastasis of tumor cells that overexpress these kinases. c-Met, VEGFR2, Axl, Mer, and Flt3 are overexpressed in various tumor cell types and play crucial roles in tumor cell proliferation, survival, invasion, and metastasis.
CT-053 tosylate is a potent, orally bioavailable small molecule tyrosine kinase inhibitor. It is also known as Ningetinib Tosylate, DE-120, and CT-053. It is used in research of cancer and wet age-related macular degeneration. It is not approved for clinical use. |
| Molecular Formula |
C38H37FN4O8S
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|---|---|
| Molecular Weight |
728.78579211235
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| Exact Mass |
728.231
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| CAS # |
1394820-77-9
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| Related CAS # |
Ningetinib;1394820-69-9
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| PubChem CID |
73442844
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
52
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| Complexity |
1190
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
NAUYISNCVNUUDK-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C31H29FN4O5.C7H8O3S/c1-19-28(30(38)36(35(19)4)21-8-6-5-7-9-21)29(37)34-20-10-13-27(24(32)16-20)41-26-14-15-33-25-17-22(11-12-23(25)26)40-18-31(2,3)39;1-6-2-4-7(5-3-6)11(8,9)10/h5-17,39H,18H2,1-4H3,(H,34,37);2-5H,1H3,(H,8,9,10)
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| Chemical Name |
N-[3-fluoro-4-[7-(2-hydroxy-2-methylpropoxy)quinolin-4-yl]oxyphenyl]-1,5-dimethyl-3-oxo-2-phenylpyrazole-4-carboxamide;4-methylbenzenesulfonic 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: Please store this product in a sealed and protected environment, 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 : ~33.33 mg/mL (~45.73 mM)
H2O : < 0.1 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.43 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 25.0 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (3.43 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (3.43 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.3721 mL | 6.8607 mL | 13.7214 mL | |
| 5 mM | 0.2744 mL | 1.3721 mL | 2.7443 mL | |
| 10 mM | 0.1372 mL | 0.6861 mL | 1.3721 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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