SRPIN803
Based on 1 Customer Validation
SRPIN803 is a potent CK2 and SRPK1 dual inhibitor, with IC50s of 203 nM and 2.4 μM, respectively. SRPIN803 exhibits antiangiogenic activity. SRPIN803 can be used for the research of age-related macular degeneration.
For research use only. We do not sell to patients.
- Purity: 99.70%
- CAS No.: 380572-02-1
- Formula: C14H9F3N4O3S
- Molecular Weight:370.31
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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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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CK2 203 nM (IC50) |
SRPK1 2.4 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HL-60 | IC50 |
44.7 μM
Compound: SRPIN803
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Cytotoxicity against HL-60 cells
Cytotoxicity against HL-60 cells
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[PMID: 35863237] |
| K562 | IC50 |
44.7 μM
Compound: SRPIN803
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Cytotoxicity against human K562 cells
Cytotoxicity against human K562 cells
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[PMID: 35863237] |
SRPIN803 inhibits the activity of SRPK1 toward LBRNt (62-92), with an IC50 of 7.5 μM, while the c(RGDyK)-conjugated compounds completely abolishes its inhibitory activity[2].
SRPIN803 has slightly cytostatic activity against Hcc827, PC3, and U87 (GI50=80-98 μM)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
SRPIN803 (100 μM; 72 h) inhibit zebrafish angiogenesis[2].
SRPIN803 (4.6 nL of 10 μM; microinjection; 72 h) block angiogenesis in the developing embryo at the one-cell stage of zebrafish[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 380572-02-1
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Appearance Solid
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Molecular Weight 370.31
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Formula C14H9F3N4O3S
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Color Light yellow to yellow
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SMILES
O=C(N=C1SC(C(F)(F)F)=NN1C/2=N)C2=C/C3=CC=C(C(OC)=C3)O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (270.04 mM; ultrasonic and warming and heat to 80°C; 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 (6.75 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
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.
Purity & Documentation
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Data Sheet (274 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Leonidis G, et, al. Synthesis and Biological Evaluation of a c(RGDyK) Peptide Conjugate of SRPIN803. ACS Omega. 2021 Oct 14;6(42):28379-28393. [Content Brief]
[2]. Vedove AD, et, al. A novel class of selective CK2 inhibitors targeting its open hinge conformation. Eur J Med Chem. 2020 Jun 1;195:112267. [Content Brief]
[3]. Morooka S, et, al. Identification of a Dual Inhibitor of SRPK1 and CK2 That Attenuates Pathological Angiogenesis of Macular Degeneration in Mice. [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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.7004 mL | 13.5022 mL | 27.0044 mL | 67.5110 mL |
| 5 mM | 0.5401 mL | 2.7004 mL | 5.4009 mL | 13.5022 mL | |
| 10 mM | 0.2700 mL | 1.3502 mL | 2.7004 mL | 6.7511 mL | |
| 15 mM | 0.1800 mL | 0.9001 mL | 1.8003 mL | 4.5007 mL | |
| 20 mM | 0.1350 mL | 0.6751 mL | 1.3502 mL | 3.3756 mL | |
| 25 mM | 0.1080 mL | 0.5401 mL | 1.0802 mL | 2.7004 mL | |
| 30 mM | 0.0900 mL | 0.4501 mL | 0.9001 mL | 2.2504 mL | |
| 40 mM | 0.0675 mL | 0.3376 mL | 0.6751 mL | 1.6878 mL | |
| 50 mM | 0.0540 mL | 0.2700 mL | 0.5401 mL | 1.3502 mL | |
| 60 mM | 0.0450 mL | 0.2250 mL | 0.4501 mL | 1.1252 mL | |
| 80 mM | 0.0338 mL | 0.1688 mL | 0.3376 mL | 0.8439 mL | |
| 100 mM | 0.0270 mL | 0.1350 mL | 0.2700 mL | 0.6751 mL |
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