MSC-1186 is a selective pan-SRPK inhibitor. MSC-1186 has activity against SRPK1, SRPK2 and SRPK3 with IC50s of 2.7 nM, 81 nM and 0.6 nM respectively. MSC-1186 may be used in cancer research.

Physicochemical Properties

Molecular Formula	C19H17CLFN7O2S
Molecular Weight	461.900383710861
Exact Mass	461.083
CAS #	2871698-23-4
PubChem CID	162368309
Appearance	White to light yellow solid powder
LogP	2.4
Hydrogen Bond Donor Count	2
Hydrogen Bond Acceptor Count	9
Rotatable Bond Count	6
Heavy Atom Count	31
Complexity	714
Defined Atom Stereocenter Count	0
SMILES	CS(N(C1=NC=CC=C1CNC1C=CN=C(C2NC3=C(F)C(Cl)=CC=C3N=2)N=1)C)(=O)=O
InChi Key	WBFJDKLBAAHKIL-UHFFFAOYSA-N
InChi Code	InChI=1S/C19H17ClFN7O2S/c1-28(31(2,29)30)19-11(4-3-8-23-19)10-24-14-7-9-22-17(26-14)18-25-13-6-5-12(20)15(21)16(13)27-18/h3-9H,10H2,1-2H3,(H,25,27)(H,22,24,26)
Chemical Name	N-[3-[[[2-(5-chloro-4-fluoro-1H-benzimidazol-2-yl)pyrimidin-4-yl]amino]methyl]pyridin-2-yl]-N-methylmethanesulfonamide
HS Tariff Code	2934.99.9001
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)

Biological Activity

Targets	IC50: 2.7 nM (SRPK1), 81 nM (SRPK2), 0.6 nM (SRPK3); EC50 in HEK293T cells: 98 nM (SRPK1), 40 nM (SRPK3)[1].
ln Vitro	In HEK293T cells, MSC-1186 exhibits activity against SRPK1 and SRPK3 with EC50 values of 98 nM and 40 nM, respectively[1]. The IC50 values of MSC-1186's activity against SRPK1, SRPK2, and SRPK3 are 2.7 nM, 81 nM, and 0.6 nM, respectively[1]. Excellent kinome-wide selectivity is possessed by MSC-1186 [1]. When CDC2-like kinase (CLK) inhibitors are employed in conjunction with MSC-1186, SR protein phosphorylation is attenuated in an additive manner [1].
References	[1]. MSC-1186, a Highly Selective Pan-SRPK Inhibitor Based on an Exceptionally Decorated Benzimidazole-Pyrimidine Core. J Med Chem. 2022 Dec 14.

Solubility Data

Solubility (In Vitro)

DMSO : 125 mg/mL (270.62 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.08 mg/mL (4.50 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to 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. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.50 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.1650 mL	10.8249 mL	21.6497 mL
	5 mM	0.4330 mL	2.1650 mL	4.3299 mL
	10 mM	0.2165 mL	1.0825 mL	2.1650 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.