| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg | |||
| Other Sizes |
| Targets |
SRPIN-803 targets CK2 and SRPK1, two kinases involved in various cellular processes including angiogenesis, cell proliferation, and splicing regulation. It is a selective dual SRPK1 and CK2 inhibitor with IC50 values of 203 nM for CK2 and 2.4 μM for SRPK1.
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| ln Vitro |
With an IC50 value of 7.5 μM, SRPIN803 suppresses SRPK1 activity on LBRNt (62–92), whereas c(RGDyK)-conjugated compounds totally eliminated its inhibitory activity [2]. A small level of cytostatic action (GI50=80-98 μM) has been seen against Hcc827, PC3, and U87 by SRPIN803[2].
SRPIN-803 is a potent CK2 and SRPK1 dual inhibitor. It exhibits IC50 values of 203 nM for CK2 and 2.4 μM for SRPK1. SRPIN-803 exhibits antiangiogenic activity. The compound's inhibition of SRPK1, which regulates alternative splicing of VEGF, contributes to its antiangiogenic effects. |
| ln Vivo |
In a mouse model of apoptosis-related macular degeneration, topical Manhattan eye ointment SRPIN803 substantially prevents choroidal neovascularization [3]. Zebrafish angiogenesis is inhibited by SRPIN803 (100 μM; 72 h)[2]. SRPIN803 microinjection (4.6 nL of 10 μM; 72 h) induces angiogenesis in foam horsefish cells growing in a single phase [2].
SRPIN-803 exhibits antiangiogenic activity in vivo. It has been investigated for the research of age-related macular degeneration, a disease characterized by pathological angiogenesis. Specific animal model data and dosing regimens are not extensively detailed in standard reference sources. |
| Enzyme Assay |
SRPIN-803's inhibitory activity against CK2 and SRPK1 can be assessed using in vitro kinase assays. Recombinant CK2 or SRPK1 enzymes are incubated with their respective substrates and ATP in the presence of varying concentrations of SRPIN-803. The amount of phosphorylated substrate is measured using a suitable detection method to determine the IC50.
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| Cell Assay |
The cellular activity of SRPIN-803 is evaluated in endothelial cell-based assays. Human umbilical vein endothelial cells (HUVECs) are treated with increasing concentrations of SRPIN-803, and angiogenesis-related processes such as cell proliferation, migration, and tube formation are assessed. The effect on VEGF-induced signaling and SRPK1-mediated splicing can also be examined.
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| Animal Protocol |
Specific in vivo animal experimental protocols for SRPIN-803 are not extensively detailed in standard reference sources. For evaluating its antiangiogenic activity, SRPIN-803 would be administered to animal models of ocular neovascularization, such as the laser-induced choroidal neovascularization (CNV) model in mice. Retinal angiogenesis and vascular leakage would be assessed.
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| ADME/Pharmacokinetics |
SRPIN-803 has a molecular formula of C14H9F3N4O3S and a molecular weight of 370.31. It is soluble in DMSO. Specific pharmacokinetic parameters such as half-life, bioavailability, and plasma protein binding are not extensively detailed in standard reference sources.
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| Toxicity/Toxicokinetics |
The toxicity profile of SRPIN-803 is not extensively documented. As a kinase inhibitor, potential adverse effects may include off-target kinase inhibition. Specific LD50 values and organ-specific toxicity data are not readily available.
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| 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.
[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. [3]. Morooka S, et, al. Identification of a Dual Inhibitor of SRPK1 and CK2 That Attenuates Pathological Angiogenesis of Macular Degeneration in Mice. |
| Additional Infomation |
SRPIN-803 (CAS# 380572-02-1) is a potent dual CK2 and SRPK1 inhibitor with IC50 values of 203 nM and 2.4 μM, respectively. It exhibits antiangiogenic activity and has been investigated for age-related macular degeneration research. The compound is a research tool for studying angiogenesis and kinase signaling.
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| Molecular Formula |
C14H9F3N4O3S
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|---|---|
| Molecular Weight |
370.3
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| Exact Mass |
370.034
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| CAS # |
380572-02-1
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| PubChem CID |
16411419
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.7±0.1 g/cm3
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| Boiling Point |
428.5±55.0 °C at 760 mmHg
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| Flash Point |
212.9±31.5 °C
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| Vapour Pressure |
0.0±1.1 mmHg at 25°C
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| Index of Refraction |
1.678
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| LogP |
1.6
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
25
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| Complexity |
865
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| Defined Atom Stereocenter Count |
0
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| SMILES |
COC1=C/C(=C/C2=C(N3C(=NC2=O)SC(=N3)C(F)(F)F)N)/C=CC1=O
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| InChi Key |
JCSNCMXWHKOYJB-GQCTYLIASA-N
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| InChi Code |
InChI=1S/C14H9F3N4O3S/c1-24-9-5-6(2-3-8(9)22)4-7-10(18)21-13(19-11(7)23)25-12(20-21)14(15,16)17/h2-5H,18H2,1H3/b6-4+
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| Chemical Name |
5-amino-6-[(E)-(3-methoxy-4-oxocyclohexa-2,5-dien-1-ylidene)methyl]-2-(trifluoromethyl)-[1,3,4]thiadiazolo[3,2-a]pyrimidin-7-one
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| Synonyms |
SRPIN803; SRPIN 803; SRPIN-803
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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 |
| 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) |
DMSO: ~100 mg/mL (~270.0 mM; with ultrasonication and warming by heating to 80°C)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (6.75 mM) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution; with ultrasonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7005 mL | 13.5026 mL | 27.0051 mL | |
| 5 mM | 0.5401 mL | 2.7005 mL | 5.4010 mL | |
| 10 mM | 0.2701 mL | 1.3503 mL | 2.7005 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.
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