SU14813
Based on 1 publication(s) in Google Scholar
SU14813 is a multi-targeted receptor tyrosine kinases inhibitor with IC50s of 50, 2, 4, 15 nM for VEGFR2, VEGFR1, PDGFRβ and KIT.
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- Pureté: 99.11%
- CAS No.: 627908-92-3
- Formule: C23H27FN4O4
- Masse moléculaire:442.48
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) SU14813
MoreVoir tous les produits spécifiques à Isoform VEGFR
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Activité biologique
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VEGFR1 2 nM (IC50) |
VEGFR2 50 nM (IC50) |
PDGFRβ 4 nM (IC50) |
KIT 15 nM (IC50) |
SU14813 inhibits ligand-dependent and ligand-independent proliferation, migration, and survival of endothelial cells and/or tumor cells expressing these targets. SU14813 inhibits cellular ligand-dependent phosphorylation of VEGFR-2 (transfected NIH 3T3 cells), PDGFR-β (transfected NIH 3T3 cells), KIT (Mo7e cells), and FLT3-internal tandem duplication (FLT3-ITD; MV4;11 cells) as well as FMS/CSF1R (transfected NIH 3T3 cells). SU14813 inhibits VEGFR-2, PDGFR-β, and KIT phosphorylation in porcine aorta endothelial cells overexpressing these targets, with cellular IC50 values of 5.2, 9.9, and 11.2 nM, respectively. SU14813 inhibits the growth of U-118MG with an IC50 of 50 to 100 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 627908-92-3
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Appearance Solid
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Masse moléculaire 442.48
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Formule C23H27FN4O4
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Color Light yellow to yellow
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SMILES
O=C(/C(C1=C2)=C/C3=C(C(C(NC[C@H](O)CN4CCOCC4)=O)=C(N3)C)C)NC1=CC=C2F
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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Science
2017 Dec 1;358(6367):eaan4368. PMID: 29191878
Solvant et solubilité
DMSO : 44 mg/mL (99.44 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.65 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocole
The effect of SU14813 on endothelial cell survival is evaluated. Passages 4 to 5 human umbilical vein endothelial cells are grown to subconfluency in EGM2 medium containing 10% FBS, endothelial cell growth supplement, and 10 μg/mL sodium heparin. The cells are seeded in 96-well plates at 10,000 per well in F12K medium and 10% FBS. The next day, cells are starved for 18 hours in F12K+1% FBS and then incubated with SU14813 in various concentrations. 45 minutes later, 20 ng/mL growth factor [VEGF or basic fibroblast growth factor (bFGF)] is introduced into the assay. Three days later, cell numbers are determined using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mouse: SU14813 is evaluated for its efficacy and synergism in combination with the microtubule inhibitor docetaxel in docetaxel-resistant murine LLC model. SU14813 is administered p.o. twice daily (BID) at doses of 10, 40, 80, or 120 mg/kg beginning on day 5 after tumor implantation. Docetaxel 40 mg/kg (mouse maximum tolerated dose) is administered i.v. thrice weekly also beginning on day 5 after tumor implantation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (276 KB)
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SDS (643 KB)
- English - EN (643 KB)
- Français - FR (643 KB)
- Deutsch - DE (643 KB)
- Norwegian - NO (643 KB)
- Español - ES (643 KB)
- Swedish - SV (643 KB)
- Italian - IT (643 KB)
- Korean - KR (643 KB)
- Portuguese - PT (643 KB)
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Instruction de manipulation (2659 KB)
Références
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2600 mL | 11.2999 mL | 22.5999 mL | 56.4997 mL |
| 5 mM | 0.4520 mL | 2.2600 mL | 4.5200 mL | 11.2999 mL | |
| 10 mM | 0.2260 mL | 1.1300 mL | 2.2600 mL | 5.6500 mL | |
| 15 mM | 0.1507 mL | 0.7533 mL | 1.5067 mL | 3.7666 mL | |
| 20 mM | 0.1130 mL | 0.5650 mL | 1.1300 mL | 2.8250 mL | |
| 25 mM | 0.0904 mL | 0.4520 mL | 0.9040 mL | 2.2600 mL | |
| 30 mM | 0.0753 mL | 0.3767 mL | 0.7533 mL | 1.8833 mL | |
| 40 mM | 0.0565 mL | 0.2825 mL | 0.5650 mL | 1.4125 mL | |
| 50 mM | 0.0452 mL | 0.2260 mL | 0.4520 mL | 1.1300 mL | |
| 60 mM | 0.0377 mL | 0.1883 mL | 0.3767 mL | 0.9417 mL | |
| 80 mM | 0.0282 mL | 0.1412 mL | 0.2825 mL | 0.7062 mL |
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