Cevidoplenib is an orally bioactive splenic tyrosine kinase (Syk) inhibitor (antagonist) with potential anti~inflammatory and Immune-modulatory effects.

Physicochemical Properties

Molecular Formula	C27H35N7O9S2
Molecular Weight	665.738303422928
Exact Mass	665.193
CAS #	2043659-93-2
Related CAS #	Cevidoplenib;1703788-21-9
PubChem CID	137528229
Appearance	Yellow to brown solid powder
Hydrogen Bond Donor Count	4
Hydrogen Bond Acceptor Count	14
Rotatable Bond Count	7
Heavy Atom Count	45
Complexity	862
Defined Atom Stereocenter Count	1
SMILES	S(C)(=O)(=O)O.S(C)(=O)(=O)O.O=C(C1=CN(C)C2C=CC(=CC1=2)NC1N=CC=C(N=1)N1C=C(C(C)=N1)CN1C[C@@H](CO1)O)C1CC1
InChi Key	KGZICKLRNSIYNH-TXEPZDRESA-N
InChi Code	InChI=1S/C25H27N7O3.2CH4O3S/c1-15-17(10-31-12-19(33)14-35-31)11-32(29-15)23-7-8-26-25(28-23)27-18-5-6-22-20(9-18)21(13-30(22)2)24(34)16-3-4-16;2*1-5(2,3)4/h5-9,11,13,16,19,33H,3-4,10,12,14H2,1-2H3,(H,26,27,28);2*1H3,(H,2,3,4)/t19-;;/m0../s1
Chemical Name	cyclopropyl-[5-[[4-[4-[[(4S)-4-hydroxy-1,2-oxazolidin-2-yl]methyl]-3-methylpyrazol-1-yl]pyrimidin-2-yl]amino]-1-methylindol-3-yl]methanone;methanesulfonic acid
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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.
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

References

[1]. International Nonproprietary Names for Pharmaceutical Substances (INN). WHO Drug Information, Vol. 31, No. 4, 2017. [2]. cevidoplenib dimesylate.

Additional Infomation

Cevidoplenib Dimesylate is the dimesylate salt of cevidoplenib, an orally available inhibitor of spleen tyrosine kinase (SYK), with potential anti-inflammatory and immunomodulating activities. Upon oral administration, cevidoplenib binds to and inhibits the activity of SYK, blocking Fc receptor and B-cell receptor (BCR)-mediated signaling in inflammatory cells, including macrophages, neutrophils, mast cells, natural killer (NK) cells and B-cells. This leads to the inhibition of the activation of these inflammatory cells, and the related inflammatory responses and tissue damage. SYK, a non-receptor cytoplasmic protein tyrosine kinase widely expressed in hematopoietic cells, plays a key role in Fc receptor and B-cell receptor signaling in inflammatory cells. It is involved in coupling activated immunoreceptors, such as Fc receptors and B-cell receptors, to signal downstream events that mediate diverse cellular responses, including proliferation, differentiation, and phagocytosis, which are important for allergic and antibody-mediated immune diseases such as immune thrombocytopenia (ITP).

Solubility Data

Solubility (In Vitro)

DMSO: 25 mg/mL (37.55 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (3.76 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 25.0 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: ≥ 2.5 mg/mL (3.76 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline 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	1.5021 mL	7.5104 mL	15.0209 mL
	5 mM	0.3004 mL	1.5021 mL	3.0042 mL
	10 mM	0.1502 mL	0.7510 mL	1.5021 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.