| Identification | Back Directory | [Name]
Methanone, cyclopropyl[5-[[4-[4-[[(4S)-4-hydroxy-2-isoxazolidinyl]methyl]-3-methyl-1H-pyrazol-1-yl]-2-pyrimidinyl]amino]-1-methyl-1H-indol-3-yl]- | [CAS]
1703788-21-9 | [Synonyms]
Cevidoplenib
Cyclopropyl[5-[[4-[4-[[(4S)-4-hydroxy-2-isoxazolidinyl]methyl]-3-methyl-1H-pyrazol-1-yl]-2-pyrimidinyl]amino]-1-methyl-1H-indol-3-yl]methanone
Methanone, cyclopropyl[5-[[4-[4-[[(4S)-4-hydroxy-2-isoxazolidinyl]methyl]-3-methyl-1H-pyrazol-1-yl]-2-pyrimidinyl]amino]-1-methyl-1H-indol-3-yl]- | [Molecular Formula]
C25H27N7O3 | [MDL Number]
MFCD34469203 | [MOL File]
1703788-21-9.mol | [Molecular Weight]
473.53 |
| Chemical Properties | Back Directory | [Boiling point ]
751.1±70.0 °C(Predicted) | [density ]
1.50±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [form ]
Solid | [pka]
13.96±0.20(Predicted) | [color ]
Off-white to gray |
| Hazard Information | Back Directory | [Uses]
Cevidoplenib (SKI-O-703) is an orally available inhibitor of spleen tyrosine kinase (Syk), with potential anti-inflammatory and immunomodulating activities. Cevidoplenib is also the mesylate form of SKI-O-592. Cevidoplenib and SKI-O-592 inhibits BCR-mediated survival, proliferation, and differentiation of B cells. And SKI-O-592 potently inhibits multiple kinases with IC50s of 6.2 nM (Syk), 1.859 μM (Jak2), 5.807 μM (Jak3), 0.412 μM (RET), 0.687 μM (KOR), 1.783 μM (FLT3), 16.96 μM (FGFR1), 5.662 μM (FGFR3), and 0.709 μM (Pyk2), respectively[1][2][3]. | [in vivo]
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[2]. | [References]
[1] Cho S, et al. A novel selective spleen tyrosine kinase inhibitor SKI-O-703 (cevidoplenib) ameliorates lupus nephritis and serum-induced arthritis in murine models. Clin Exp Immunol. 2023 Mar 8;211(1):31-45. DOI:10.1093/cei/uxac096
[2] International Nonproprietary Names for Pharmaceutical Substances (INN). WHO Drug Information, Vol. 31, No. 4, 2017.
[3] cevidoplenib dimesylate. |
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DC Chemicals
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