Cevidoplenib (Synonyms: SKI-O-703) |
| Catalog No.GC63429 |
Cevidoplenib (SKI-O-703) is an orally active and selective spleen tyrosine kinase (Syk) inhibitor.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1703788-21-9
Sample solution is provided at 25 µL, 10mM.
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Cevidoplenib (SKI-O-703) is an orally active and selective spleen tyrosine kinase (Syk) inhibitor[1]. Syk is a crucial regulatory molecule in the signal transduction pathways involved in autoimmune diseases such as immune thrombocytopenia (ITP)[2]. Cevidoplenib is also the mesylate form of SKI-O-592, with an IC50 value of 6.2 nM for Syk[3].
In vitro, Cevidoplenib (0-5μM) treated primary mouse B cells for 72 hours, inhibiting B cell receptor (BCR) cross-linking-induced cell proliferation in a concentration-dependent manner. It increased the proportion of early and late apoptotic cells. This cytotoxic effect was stronger when B cells were activated by anti-IgM mAb compared to LPS activation[3].
In vivo, Cevidoplenib (84 mg/kg) was administered orally to mice with systemic lupus erythematosus (SLE), significantly reducing levels of IgG autoantibodies, proteinuria, and glomerulonephritis. It also decreased the levels of germinal centers (GC) involved in humoral immune responses and serum B cell-activating factor (BAFF) signaling from the TNF family[3]. Cevidoplenib (42, 84 mg/kg) was administered orally to mice with antiphospholipid syndrome (APS), significantly reducing antiphospholipid antibody (APLs) levels and preventing myocardial arteriolar thrombosis in mice[4]. Cevidoplenib (10 mg/kg) was administered orally to mice with alcoholic liver disease (ALD), effectively reducing hepatic neutrophil infiltration, inhibiting liver injury, and steatosis[5].
References:
[1] Provan D, Newland A C. Investigational drugs for immune thrombocytopenia[J]. Expert Opinion on Investigational Drugs, 2022, 31(7): 715-727.
[2] Cooper N, Ghanima W, Hill Q A, et al. Recent advances in understanding spleen tyrosine kinase (SYK) in human biology and disease, with a focus on fostamatinib[J]. Platelets, 2023, 34(1): 2131751.
[3] Cho S, Jang E, Yoon T, et al. A novel selective spleen tyrosine kinase inhibitor SKI-O-703 (cevidoplenib) ameliorates lupus nephritis and serum-induced arthritis in murine models[J]. Clinical and Experimental Immunology, 2023, 211(1): 31-45.
[4] Jang E, Hwang H, Yoon T, et al. S307: CEVIDOPLENIB (SKI-O-703), A NOVEL SYK INHIBITOR, REDUCES ANTIPHOSPHOLIPID ANTIBODY TITERS AND PREVENTS INTRAMYOCARDIAL SMALL ARTERIAL THROMBOSIS IN A MOUSE MODEL OF ANTIPHOSPHOLIPID SYNDROME[J]. HemaSphere, 2023, 7(S3): e3562913.
[5] Kim J W, Roh Y S, Jeong H, et al. Spliceosome-associated protein 130 exacerbates alcohol-induced liver injury by inducing NLRP3 inflammasome–mediated IL-1β in mice[J]. The American journal of pathology, 2018, 188(4): 967-980.
Cell experiment [1]: | |
Cell lines | Mouse primary B cells |
Preparation method | Mouse primary B cells were labeled with CP670, and stimulated with either anti-IgM mAb, CD40L and IL-4 or LPS for 72 h in the presence or absence of Cevidoplenib (0-5μM) and tofacitinib at the indicated concentrations. |
Reaction Conditions | 0-5μM; 72 h |
Applications | Cevidoplenib inhibits B-cell receptor (BCR) cross-linking-induced cell proliferation in a concentration-dependent manner. |
Animal experiment [2]: | |
Animal models | Male WT or Mincle KO mice |
Preparation method | After control diet feeding for 5 days, mice received 10 mg/kg Cevidoplenib or vehicle control by oral administration every 10 days during EtOH-diet feeding. |
Dosage form | 10mg/kg; p.o. |
Applications | EtOH-fed mice treated with Cevidoplenib had reduced liver neutrophil infiltration, liver damage, and steatosis. |
References: | |
| Cas No. | 1703788-21-9 | SDF | |
| Synonyms | SKI-O-703 | ||
| Formula | C25H27N7O3 | M.Wt | 473.53 |
| Solubility | DMSO:35 mg/mL | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.1118 mL | 10.559 mL | 21.118 mL |
| 5 mM | 0.4224 mL | 2.1118 mL | 4.2236 mL |
| 10 mM | 0.2112 mL | 1.0559 mL | 2.1118 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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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.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 3 reference(s) in Google Scholar.)
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