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Purity: ≥98%
SPHINX31 is a novel, highly potent, selective, and cell bioactive inhibitor of the serine/arginine-rich protein kinase 1 (SRPK1) with IC50 value of 6 nM. Serine/arginine splicing factor 1 (SRSF1) was phosphorylated and SRPK1 activity was inhibited by SPHINX31 treatment. This led to alternative splicing of VEGF-A, which changed its pro-angiogenic isoform to an antiangiogenic one. SPHINX31 raises expression of the anti-angiogenic VEGF-A165b splice variant in retinal pigment epithelial (RPE) cells and inhibits phosphorylation of serine/arginine-rich splicing factor 1 (SRSF1), an SRPK1 substrate, in PC3 cells (EC50 = 360 nM). In a mouse model of choroidal neovascularization, SPHINX31 (2 μg per eye) prevents the growth of blood vessels and the infiltration of macrophages into the eyes. The regulation of VEGF-A alternative splicing to pro-angiogenic isoforms is carried out by serine/arginine-protein kinase 1 (SRPK1), and inhibition of SRPK1 can return the balance between pro- and antiangiogenic isoforms to normal physiological levels.
| Targets |
SRPK1 (IC50 = 5.9 nM); VEGF-A165a
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|---|---|
| ln Vitro |
SPHINX31 was identified as a type 1 kinase inhibitor (ATP competitive) by kinase assays. In PC3 prostate cancer cells, SPHINX31 treatment inhibits SRSF1 phosphorylation at 300 nM. According to mouse liver microsome metabolic stability, SPHINX31 exhibited a medium clearance with a T1/2 of 95.79 min[1]. Leukemic cell differentiation and cell cycle arrest result from SPHINX31-mediated SRPK1 inhibition[2].
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| ln Vivo |
SPHINX31 has the potential to enter the eye. In a mouse model, SPHINX31 inhibits choroidal neovascularization in a dose-dependent manner. SPHINX31 prevents macrophage infiltration and blood vessel growth[1]. Immunocompromised mice receiving transplants of MLL-rearranged AML cells have longer survival times when treated with SPHINX31[2].
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| Animal Protocol |
DBA2J mice
0.8 mg/kg i.p. |
| References |
| Molecular Formula |
C27H24F3N5O2
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|---|---|
| Molecular Weight |
507.51
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| Exact Mass |
507.19
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| Elemental Analysis |
C, 63.90; H, 4.77; F, 11.23; N, 13.80; O, 6.30
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| CAS # |
1818389-84-2
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| Related CAS # |
1818389-84-2
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| Appearance |
Solid powder
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| SMILES |
C1CN(CCN1CC2=CC=CC=N2)C3=C(C=C(C=C3)C(F)(F)F)NC(=O)C4=CC=C(O4)C5=CC=NC=C5
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| InChi Key |
VURLRACCOCGFDB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C27H24F3N5O2/c28-27(29,30)20-4-5-23(35-15-13-34(14-16-35)18-21-3-1-2-10-32-21)22(17-20)33-26(36)25-7-6-24(37-25)19-8-11-31-12-9-19/h1-12,17H,13-16,18H2,(H,33,36)
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| Chemical Name |
5-pyridin-4-yl-N-[2-[4-(pyridin-2-ylmethyl)piperazin-1-yl]-5-(trifluoromethyl)phenyl]furan-2-carboxamide
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| Synonyms |
SPHINX31; SPHINX 31; SPHINX-31
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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: 17.3~25 mg/mL (49.3~34.2 mM)
Ethanol: ~13 mg/mL (~25.6 mM) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9704 mL | 9.8520 mL | 19.7040 mL | |
| 5 mM | 0.3941 mL | 1.9704 mL | 3.9408 mL | |
| 10 mM | 0.1970 mL | 0.9852 mL | 1.9704 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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