| Size | Price | Stock | Qty |
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| 10mg |
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| Targets |
SPHINX targets serine/arginine-rich protein kinase 1 (SRPK1), a kinase that phosphorylates serine/arginine-rich (SR) proteins involved in pre-mRNA splicing and other RNA processing events. SRPK1 plays a role in angiogenesis by regulating the splicing of vascular endothelial growth factor (VEGF) isoforms. By inhibiting SRPK1 with an IC50 of 0.58-0.88 µM, SPHINX modulates VEGF splicing, reducing the production of pro-angiogenic VEGF isoforms.
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| ln Vitro |
SRSF1 and SRSF2 phosphorylation generated by EGF is affected by SPHINX (10 μM; 2 hours) [1]. SPHINX (5 μM; 24 hours) lowers VEGF165 expression in primary RPE and ARPE-19 cell lines as compared to GAPDH control [1].
In vitro, SPHINX inhibits SRPK1 with an IC50 of 0.58 µM (or 0.88 µM in some reports). It is selective for SRPK1 over SRPK2 (IC50 >10 µM). The compound's potent and selective SRPK1 inhibition makes it a valuable tool for studying the role of SRPK1 in RNA processing, angiogenesis, and disease. It can be used to investigate the mechanisms underlying choroidal neovascularization and other angiogenesis-related conditions. |
| ln Vivo |
SPHINX (10 ng; io on days 0 and 7 of laser photocoagulation) affects the growth of new blood vessels in vivo [1]. SPHINX (25 ng; io on days 0 and 7 of laser photocoagulation) affects CNV area in CNV rats [1].
In vivo, SPHINX effectively reduces choroidal neovascularization (CNV) in animal models. This supports its potential for studying age-related macular degeneration, a condition characterized by abnormal blood vessel growth in the eye. By inhibiting SRPK1 and modulating VEGF splicing, SPHINX reduces the production of pro-angiogenic VEGF isoforms, leading to decreased neovascularization. The compound's in vivo efficacy in CNV models makes it a promising research tool for studying angiogenesis and related diseases. |
| Enzyme Assay |
For in vitro kinase assays, recombinant SRPK1 protein is incubated with a peptide substrate (such as an SR protein-derived peptide) and ATP in kinase assay buffer. The test compound is added at various concentrations (typically 0.001-100 µM). Kinase activity is measured using radioactive ATP incorporation or using non-radioactive methods such as luminescent ADP detection assays. IC50 values are calculated by fitting dose-response curves.
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: ARPE-19 Cell Line Tested Concentrations: 10 μM Incubation Duration: 2 hrs (hours) Experimental Results: Blocks EGF-induced phosphorylation of SRSF1 and SRSF2. For cell-based assays, cells are treated with SPHINX at concentrations ranging from 0.01-10 µM for various time points. SRPK1 activity is assessed by measuring the phosphorylation of SR proteins by Western blotting with phospho-SR protein-specific antibodies. VEGF isoform expression can be assessed by RT-PCR or Western blotting to evaluate the effects of SRPK1 inhibition on alternative splicing. Cell proliferation, migration, and angiogenesis assays can also be performed. |
| Animal Protocol |
Animal/Disease Models: C57/B6 mice with laser-induced CNV [1]
Doses: 10 ng Route of Administration: intraocular injection; laser photocoagulation 10 ng on days 0 and 7 Experimental Results: Compared with the control injected with normal saline, New blood vessel growth was Dramatically diminished. Animal/Disease Models: Norwegian brown rats, laser-induced choroidal neovascularization [1] Doses: 25 ng (10 ng/uL) Route of Administration: intraocular injection; laser photocoagulation on days 0 and 7 is 25 ng (10 ng/uL) Experimental Results: CNV area was Dramatically diminished compared to saline-injected controls. For in vivo efficacy studies, the laser-induced choroidal neovascularization (CNV) model in mice or rats is commonly used. Laser photocoagulation is applied to the retina to induce CNV. Animals are treated with SPHINX via intraperitoneal, oral, or intravitreal administration at doses determined from pharmacokinetic studies. CNV area is measured by fluorescein angiography or by staining of choroidal flat mounts with isolectin B4. The compound's ability to reduce CNV area is quantified. |
| ADME/Pharmacokinetics |
Pharmacokinetic properties of SPHINX have not been fully characterized in the available literature. The compound has a molecular weight of 354.32 g/mol, suggesting potential for drug-like properties. Standard PK studies including solubility, permeability, half-life, oral bioavailability, and tissue distribution would be required for further development. The compound is typically stored at -20°C for long-term stability.
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| Toxicity/Toxicokinetics |
Toxicological data for SPHINX have not been extensively reported in the available literature. As a research compound, it is intended for laboratory use only and is not for human or veterinary use. Standard safety precautions should be followed when handling this compound. Comprehensive toxicology studies would be required before any clinical development.
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| References | |
| Additional Infomation |
SPHINX is a selective SRPK1 inhibitor with an IC50 of 0.58 µM (or 0.88 µM). It effectively reduces choroidal neovascularization (CNV) in vivo. SPHINX is selective for SRPK1 over SRPK2 (IC50 >10 µM). It may be utilized to study age-related macular degeneration. SPHINX is a research tool and is not approved for clinical use.
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| Molecular Formula |
C17H17F3N2O3
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|---|---|
| Molecular Weight |
354.323694944382
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| Exact Mass |
354.119
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| Elemental Analysis |
C, 57.63; H, 4.84; F, 16.09; N, 7.91; O, 13.55
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| CAS # |
848057-98-7
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| PubChem CID |
4799939
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
391.2±42.0 °C at 760 mmHg
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| Flash Point |
190.4±27.9 °C
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| Vapour Pressure |
0.0±0.9 mmHg at 25°C
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| Index of Refraction |
1.555
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| LogP |
4.01
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
25
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| Complexity |
469
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(C1=CC=C(C)O1)NC1C(N2CCOCC2)=CC=C(C(F)(F)F)C=1
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| InChi Key |
FZCPNRVICXFZJR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H17F3N2O3/c1-11-2-5-15(25-11)16(23)21-13-10-12(17(18,19)20)3-4-14(13)22-6-8-24-9-7-22/h2-5,10H,6-9H2,1H3,(H,21,23)
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| Chemical Name |
5-methyl-N-[2-morpholin-4-yl-5-(trifluoromethyl)phenyl]furan-2-carboxamide
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| Synonyms |
SPHINX
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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 : ~50 mg/mL (~141.12 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8223 mL | 14.1115 mL | 28.2231 mL | |
| 5 mM | 0.5645 mL | 2.8223 mL | 5.6446 mL | |
| 10 mM | 0.2822 mL | 1.4112 mL | 2.8223 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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