| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| Targets |
Spleen tyrosine kinase (SYK). Cevidoplenib is a SYK inhibitor. SYK is a critical signaling node in B-cell receptor (BCR) and Fc receptor (FcR) pathways, making it a key target in antibody-mediated autoimmune diseases. Cevidoplenib is an orally bioavailable, small-molecule inhibitor of spleen tyrosine kinase (SYK).
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| ln Vitro |
Cevidoplenib is a SYK inhibitor with potential anti-inflammatory and immunomodulating activities. It inhibits SYK signaling, which is involved in B-cell and Fc receptor-mediated immune responses. It is being studied for the treatment of autoimmune diseases. Cevidoplenib inhibits SYK signaling, which is involved in B-cell and Fc receptor-mediated immune responses.
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| ln Vivo |
Following oral treatment, cevidoplenib binds to SYK and inhibits its activity, preventing inflammatory cells such as mast cells, neutrophils, macrophages, and natural killer cells from signaling through the Fc and B-cell receptors (BCR). (NK) and B lymphocytes. 2].
Cevidoplenib is an orally active compound under investigation for the treatment of autoimmune and inflammatory diseases. Its in vivo efficacy has been studied in preclinical models of these diseases. Cevidoplenib is under investigation for the treatment of autoimmune and inflammatory diseases, including immune thrombocytopenia (ITP) and rheumatoid arthritis. |
| Enzyme Assay |
Specific protocols for in vitro enzyme assays for Cevidoplenib are not detailed. As a kinase inhibitor, its activity is assessed using biochemical kinase assays that measure the inhibition of SYK enzymatic activity.
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| Cell Assay |
Cellular assays for Cevidoplenib involve treating immune cells with the compound and measuring its effects on BCR and FcR signaling pathways. Its anti-inflammatory and immunomodulating effects are assessed in these assays. Cevidoplenib inhibits SYK signaling, which is involved in B-cell and Fc receptor-mediated immune responses.
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| Animal Protocol |
In vivo animal model protocols for Cevidoplenib involve its administration to animal models of autoimmune diseases, such as ITP and rheumatoid arthritis, to study its efficacy. Cevidoplenib is under investigation for the treatment of autoimmune and inflammatory diseases, including immune thrombocytopenia (ITP) and rheumatoid arthritis.
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| ADME/Pharmacokinetics |
Cevidoplenib is an orally bioavailable compound. Specific pharmacokinetic data is not available in the provided references.
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| Toxicity/Toxicokinetics |
Specific toxicological data for Cevidoplenib is not available in the provided references. As an investigational drug, its safety profile is being evaluated in clinical trials.
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| References |
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| Additional Infomation |
Cevidoplenib is an orally administered spleen tyrosine kinase (SYK) inhibitor with potential anti-inflammatory and immunomodulatory activities. After oral administration, cevidoplenib binds to SYK and inhibits its activity, thereby 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 suppression of activation of these inflammatory cells and reduces associated inflammatory responses and tissue damage. SYK is a non-receptor cytoplasmic protein tyrosine kinase widely expressed in hematopoietic cells and plays a crucial role in Fc receptor and B cell receptor signaling in inflammatory cells. It is involved in coupling activated immune receptors, such as Fc receptors and B cell receptors, to downstream signals that mediate various cellular responses, including proliferation, differentiation, and phagocytosis, which are important for allergic diseases and antibody-mediated immune diseases, such as immune thrombocytopenic purpura (ITP).
Cevidoplenib is an investigational drug not yet approved for clinical use. It is a SYK inhibitor being developed for the treatment of autoimmune diseases. Cevidoplenib (CAS#: 1703788-21-9) is an orally bioavailable, small-molecule inhibitor of spleen tyrosine kinase (SYK). |
| Molecular Formula |
C25H27N7O3
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|---|---|
| Molecular Weight |
473.526984453201
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| Exact Mass |
473.217
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| CAS # |
1703788-21-9
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| Related CAS # |
Cevidoplenib dimesylate;2043659-93-2
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| PubChem CID |
91754477
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| Appearance |
Off-white to gray solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
751.1±70.0 °C at 760 mmHg
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| Flash Point |
408.0±35.7 °C
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| Vapour Pressure |
0.0±2.6 mmHg at 25°C
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| Index of Refraction |
1.761
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| LogP |
-0.12
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
35
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| Complexity |
769
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CC1=NN(C=C1CN2C[C@@H](CO2)O)C3=NC(=NC=C3)NC4=CC5=C(C=C4)N(C=C5C(=O)C6CC6)C
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| InChi Key |
YCZUBLQESBVOSH-IBGZPJMESA-N
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| InChi Code |
InChI=1S/C25H27N7O3/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/h5-9,11,13,16,19,33H,3-4,10,12,14H2,1-2H3,(H,26,27,28)/t19-/m0/s1
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| 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
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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 : ~50 mg/mL (~105.59 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.28 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 (5.28 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. 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 | 2.1118 mL | 10.5590 mL | 21.1180 mL | |
| 5 mM | 0.4224 mL | 2.1118 mL | 4.2236 mL | |
| 10 mM | 0.2112 mL | 1.0559 mL | 2.1118 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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