2. Protein Tyrosine Kinase/RTK
  3. FGFR
  4. 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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SUN13837

SUN13837 構造式

CAS 番号 : 1080650-67-4

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SUN13837 関連抗体

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製品説明

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[1][2][3].

体外実験

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.

SUN13837 関連抗体

Cell Proliferation Assay[3]

Cell Line: SW1353 human chondrosarcoma cells, Swiss 3T3 mouse embryo fibroblast cells
Concentration: 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, 30 μM
Incubation Time: 22-23 h
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.

Western Blot Analysis[3]

Cell Line: Swiss 3T3 mouse embryo fibroblast cells
Concentration: 10 μM
Incubation Time: 16 h
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.
Parmacokinetics
Species Dose Route T1/2 CL Vd AUC0-∞ Cmax
Rat[2] 1 mg/kg i.v. 1.4 h 2.5 L/h/kg 2.3 L/kg / /
Rat[2] 10 mg/kg p.o. / / / 3704 ng·h/mL 70 ng/mL
体内実験

SUN13837 (1 mg/kg; p.o.; daily; 10 days) significantly enhances recovery of coordinated movement in a rat acute stroke model, with efficacy comparable to analog compound 17 despite compound 17 having 6-fold higher estimated brain concentration[2].
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.

Animal Model: Slc: SD (female, 180-250 g, T9 spinal cord contusion injury model)[3]
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)
Administration: i.v.; daily; 10 days
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.
臨床実験
分子量

383.49

分子式

C21H29N5O2
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

CC1=NC(OCC(N(C2CCN(CC2)CC3=CC=CC=C3)C)=O)=NC(C)=C1N
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6076 mL 13.0381 mL 26.0763 mL
5 mM 0.5215 mL 2.6076 mL 5.2153 mL
10 mM 0.2608 mL 1.3038 mL 2.6076 mL
View the 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.

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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.

  • Protocol 1

    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.
  • Protocol 2

    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.
In Vivo Dissolution Calculator
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
純度とドキュメンテーション
参考文献

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
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
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SUN13837 Related Classifications

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SUN138371080650-67-4SUN 13837SUN-13837FGFRFibroblast growth factor receptorglutamate-induced neuronal cell deathembryonic rat cerebrocortical neuronsbasic fibroblast growth factorfibroblast growth factor receptoracute cervical spinal cord injuryembryonic rat hippocampal neuronsCaco-2 cell monolayersspinal cord injurysevere spinal cord injuryCYP3A4Inhibitorinhibitorinhibit

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