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SPHINX31 Serine/threonin kinase inhibitor

Name: SPHINX31
Brand: Selleck Chemicals
SKU: S8810
Availability: InStock
Rating: 5 (2 reviews)

Cat.No.S8810

SPHINX31 is a SRPK1 inhibiror with an IC50 of 5.9 nM with highly selectivity for SRPK1 over SRPK2 (50-fold) and CLK1 (100-fold).

Chemical Structure

Molecular Weight: 507.51

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Quality Control

Batch: S881001 DMSO]25 mg/mL]false]Ethanol]13 mg/mL]false]Water]Insoluble]false Purity: 99.62%

Cited in Nature Medicine for its top-tier quality
COA
NMR
HPLC
SDS
Datasheet

99.62

Related Targets	EGFR VEGFR PDGFR FGFR c-Met Src MEK CSF-1R FLT3 HER2
Other Serine/threonin kinase Products	WNK463 SRPIN340 Benzamidine HCl GCN2iB DCLK1-IN-1 WNK-IN-11 14-3-3 η Antibody [G4H24] MKI-1 STK16-IN-1 2OH-BNPP1

Solubility

In vitro
Batch:

DMSO : 25 mg/mL (49.26 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 13 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.250mg/ml (2.46mM)	Taking the 1 mL working solution as an example, add 50 μL of 25 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.200mg/ml (0.39mM)	Taking the 1 mL working solution as an example, add 50 μL of 4 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	507.51	Formula	C₂₇H₂₄F₃N₅O₂	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	1818389-84-2	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			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

Mechanism of Action

Targets/IC₅₀/Ki	SRPK1 (Cell-free assay) 5.9 nM
In vitro	Kinase assays showed that SPHINX31 is a type 1 kinase inhibitor (ATP competitive). This compound treatment results in inhibition of SRSF1 phosphorylation at 300 nM in PC3 prostate cancer cells. Metabolic stability in mouse liver microsomes shows that this chemical had medium clearance with a T_1/2 of 95.79 min. Inhibition of SRPK1 using this inhibitor leads to cell cycle arrest and leukemic cell differentiation.
In vivo	SPHINX31 could penetrate into the eye. This compound exerts a dose dependent inhibition of choroidal neovascularisation in mouse model. It inhibits blood vessel growth and macrophage infiltration. This chemical treatment prolongs survival of immunocompromised mice transplanted with MLL-rearranged AML cells.
References	[1] https://pubmed.ncbi.nlm.nih.gov/28135068/ [2] https://pubmed.ncbi.nlm.nih.gov/30568163/

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