| Size | Price | Stock | Qty |
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| 5mg |
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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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| Other Sizes |
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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].
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| 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].
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| References | |
| Additional Infomation |
Ningetinib Tosylate is the tosylate salt form of ningetinib, an orally available inhibitor of the receptor tyrosine kinases 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), with antineoplastic activity. Upon administration, ningetinib binds to a variety of kinases, including c-Met, VEGFR2, Axl, Mer and Flt3, thereby inhibiting their signaling pathways. This inhibits growth, angiogenesis and metastasis of tumor cells that overexpress these kinases. c-Met, VEGFR2, Axl, Mer and Flt3 are overexpressed by many tumor cell types and play key roles in tumor cell proliferation, survival, invasion and metastasis.
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| 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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