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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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SKLB610 is a novel multi-targeted kinase inhibitor with more potent inhibition of VEGFR2. It has potential anticancer activity by potently suppressing human tumor angiogenesis. Because it effectively inhibits the angiogenesis of human tumors, it may have anticancer effects. At a concentration of 10μM in biochemical kinase tests, it inhibits angiogenesis-related tyrosine kinase VEGFR2, fibroblast growth factor receptor 2 (FGFR2), and platelet-derived growth factor receptor (PDGFR) at rates of 97%, 65%, and 55%, respectively. Following SKLB610 treatment, VEGF-stimulated phosphorylation of VEGFR2 in HUVECs is inhibited in a dose-dependent manner. HUVECs' capillary tube formation is significantly inhibited by SKLB610 in a concentration-dependent manner. It would be worthwhile to look into its potential as an anticancer agent.
Targets |
VEGFR2; FGFR2; PDGFR; PDGFR; FGFR2
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ln Vitro |
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ln Vivo |
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Enzyme Assay |
SKLB610 has an IC50 value of 2.2μM and selectively inhibits proliferation induced by VEGF. SKLB610 has an IC50 value of 4.7μM and a 2-fold selectivity in inhibiting VEGF-induced proliferation in HUVECs as opposed to bFGF-induced proliferation. Following SKLB610 treatment, phosphorylation of VEGFR2 stimulated by VEGF is blocked in HUVECs in a dose-dependent manner. In a concentration-dependent manner, SKLB610 significantly inhibits the formation of capillary tubes in HUVECs. At 2.5 μM, SKLB610 prevents the development of structures resembling vessels.
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Cell Assay |
The proliferation of human umbilical vein endothelial cells (HUVECs) stimulated by VEGF was more selectively inhibited by SKLB610, and this effect was linked to a decrease in the phosphorylation of VEGFR2 and p42/44 mitogen-activated protein kinase (p42/44 MAPK).
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Animal Protocol |
Female BALB/c nude mice implanted with HCT116 and A549 cells
50 mg/kg/day IP |
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References |
Molecular Formula |
C21H16F3N3O3
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Molecular Weight |
415.37
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Exact Mass |
415.11
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Elemental Analysis |
C, 60.72; H, 3.88; F, 13.72; N, 10.12; O, 11.56
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CAS # |
1125780-41-7
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Related CAS # |
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Appearance |
white solid powder
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SMILES |
CNC(=O)C1=NC=CC(=C1)OC2=CC=C(C=C2)NC(=O)C3=CC(=CC=C3)C(F)(F)F
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InChi Key |
WACDHHMEVMSODJ-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C21H16F3N3O3/c1-25-20(29)18-12-17(9-10-26-18)30-16-7-5-15(6-8-16)27-19(28)13-3-2-4-14(11-13)21(22,23)24/h2-12H,1H3,(H,25,29)(H,27,28)
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Chemical Name |
N-methyl-4-[4-[[3-(trifluoromethyl)benzoyl]amino]phenoxy]pyridine-2-carboxamide
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Synonyms |
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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 |
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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) |
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 | 2.4075 mL | 12.0375 mL | 24.0749 mL | |
5 mM | 0.4815 mL | 2.4075 mL | 4.8150 mL | |
10 mM | 0.2407 mL | 1.2037 mL | 2.4075 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.