SUN13837
SUN13837 is an orally active, blood-brain barrier permeable FGFR modulator and neuroprotective agent. SUN13837 mimics the activity of basic fibroblast growth factor, stimulates intracellular tyrosine phosphorylation of FGFR and signal transduction in neuronal cells, induces neurite outgrowth, and inhibits glutamate-induced neuronal death. SUN13837 can be used in research related to acute cervical spinal cord injury and severe spinal cord injury.
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- Pureza: 99.18%
- No. CAS: 1080650-67-4
- Fòrmula: C21H29N5O2
- Peso molecular:383.49
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
SUN13837 (10 μM; 24 h pre-incubation before glutamate exposure) exhibits 100% neuroprotective activity against glutamate-induced cell death in rat embryonic cerebral cortex and hippocampal neurons[2].
SUN13837 (10 μM; 30 min pre-incubation) inactivates CYP3A4 in a mechanism-based manner in liver microsomes, with residual activity of 60%[2].
SUN13837 (10 μM; 120 min) is a substrate of P-gp, with an efflux ratio of 6.3 in Caco-2 cell monolayers[2].
SUN13837 (100 μM; 60 min) undergoes hydrolysis by liver microsomes at a rate of 7.2 pmol/min/mg protein[2].
SUN13837 (0.3-3 μM) potently induces axonal growth in primary hippocampal neurons from E18 Wistar rats. The effect produced by 3 μM SUN13837 is comparable to that of 3 ng/mL bFGF, and significant increases in axon length are observed at concentrations of 0.3 μM and 3 μM[3].
SUN13837 (0.1-1 μM) protects primary hippocampal neurons from E18 Wistar rats against glutamate-induced cell death by activating FGFR-1, with significant neuroprotective effects observed at concentrations of 0.1 μM, 0.3 μM and 1 μM[3].
SUN13837 (0.3-3 μM; 40 minutes) activates intracellular tyrosine phosphorylation via human FGFR-1 in transfected L6 rat skeletal muscle cells, with significant elevations observed at concentrations of 0.3 μM, 1 μM and 3 μM[3].
SUN13837 (0.1-30 μM; 22-23 h) does not induce proliferation in SW1353 chondrosarcoma cells or Swiss 3T3 mouse embryonic fibroblasts, even at concentrations as high as 30 μM[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SW1353 human chondrosarcoma cells, Swiss 3T3 mouse embryo fibroblast cells
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Concentration:0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, 30 μM
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Incubation Time:22-23 h
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Result:Did not produce a significant increase in BrdU uptake in either SW1353 or Swiss 3T3 cells, with absorbance values remaining comparable to vehicle control levels.
Contrasted with bFGF, which significantly increased BrdU uptake in both cell lines.
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Cell Line:Swiss 3T3 mouse embryo fibroblast cells
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Concentration:10 μM
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Incubation Time:16 h
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Result:Had no significant effect on cyclin D1 expression.
Had no significant effect on p27(kip1) expression.
Contrasted with bFGF, which increased cyclin D1 expression by 4.6-fold and decreased p27(kip1) expression to 5% of control levels.
Systemic administration of SUN13837 (0.3-1 mg/kg; i.v.; daily; 10 days) starting up to 12 hours post-spinal cord injury significantly enhances hind limb motor function recovery (BBB score >12 at 8 weeks) and axon regeneration in rats without adverse events[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Slc: SD (female, 180-250 g, T9 spinal cord contusion injury model)[3]
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Dosage:0.3 mg/kg (first dose 90 mins post-injury); 1 mg/kg (first dose 90 mins post-injury); 1 mg/kg (first dose 12 hours post-injury)
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Administration:i.v.; daily; 10 days
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Result:Showed significantly enhanced hind limb motor function from 2 weeks post-injury onward, reaching a BBB score >12 at 8 weeks (p = 0.017), compared to vehicle group's score of 8.
Shortened MEP latency significantly (p = 0.0146) and increased MEP amplitude relative to vehicle.
Had higher BBB scores than vehicle at all time points, but the difference did not reach statistical significance (p = 0.118).
Showed significantly enhanced motor function recovery from 5 weeks post-injury onward, with a significant difference at 8 weeks (p = 0.025).
Increased 5-HT-positive area 4 mm caudal to the contusion epicenter significantly (p = 0.0043 for 90-minute group, p = 0.027 for 12-hour group) relative to vehicle.
Induced extensive caudal extension of corticospinal tract axons through the contusion site into lumbo-sacral spinal segments, whereas axon extension was limited to distal stumps in vehicle-treated rats.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1080650-67-4
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Appearance Solid
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Peso molecular 383.49
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Fòrmula C21H29N5O2
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Color White to off-white
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SMILES
CC1=NC(OCC(N(C2CCN(CC2)CC3=CC=CC=C3)C)=O)=NC(C)=C1N
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 50 mg/mL (130.38 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (6.52 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.52 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Pureza y Documentación
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Ficha de datos (277 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[2]. Sakai H, et al. Fibroblast growth factor receptor modulators employing diamines with reduced phospholipidosis-inducing potential. Bioorg Med Chem. 2020;28(14):115562. [Content Brief]
[3]. Imagama S, et al. Systemic treatment with a novel basic fibroblast growth factor mimic small-molecule compound boosts functional recovery after spinal cord injury. PLoS One. 2020;15(7):e0236050. Published 2020 Jul 17. [Content Brief]
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.6076 mL | 13.0381 mL | 26.0763 mL | 65.1907 mL |
| 5 mM | 0.5215 mL | 2.6076 mL | 5.2153 mL | 13.0381 mL | |
| 10 mM | 0.2608 mL | 1.3038 mL | 2.6076 mL | 6.5191 mL | |
| 15 mM | 0.1738 mL | 0.8692 mL | 1.7384 mL | 4.3460 mL | |
| 20 mM | 0.1304 mL | 0.6519 mL | 1.3038 mL | 3.2595 mL | |
| 25 mM | 0.1043 mL | 0.5215 mL | 1.0431 mL | 2.6076 mL | |
| 30 mM | 0.0869 mL | 0.4346 mL | 0.8692 mL | 2.1730 mL | |
| 40 mM | 0.0652 mL | 0.3260 mL | 0.6519 mL | 1.6298 mL | |
| 50 mM | 0.0522 mL | 0.2608 mL | 0.5215 mL | 1.3038 mL | |
| 60 mM | 0.0435 mL | 0.2173 mL | 0.4346 mL | 1.0865 mL | |
| 80 mM | 0.0326 mL | 0.1630 mL | 0.3260 mL | 0.8149 mL | |
| 100 mM | 0.0261 mL | 0.1304 mL | 0.2608 mL | 0.6519 mL |
SUN13837 Related Classifications
HY-147681 Related Classifications
Powered by Bioz
- SUN13837
- 1080650-67-4
- SUN 13837
- SUN-13837
- FGFR
- glutamate-induced neuronal cell death
- embryonic rat cerebrocortical neurons
- basic fibroblast growth factor
- fibroblast growth factor receptor
- acute cervical spinal cord injury
- embryonic rat hippocampal neurons
- Caco-2 cell monolayers
- spinal cord injury
- severe spinal cord injury
- CYP3A4
- Inhibitor
- inhibitor
- inhibit