Chemical Structure : NMS-0963
CAS No.:
2765304-82-1
NMS-0963
(NMS0963)
Catalog No.: PC-22156Not For Human Use, Lab Use Only.
NMS-0963 (NMS0963) is a potent, selective spleen tyrosine kinase (SYK) inhibitor with biochemical IC50 of 3 nM, inhibits SYK kinase activity in SYK-dependent BaF3-TEL/SYK cells with IC50 of 27 nM.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
NMS-0963 (NMS0963) is a potent, selective spleen tyrosine kinase (SYK) inhibitor with biochemical IC50 of 3 nM, inhibits SYK kinase activity in SYK-dependent BaF3-TEL/SYK cells with IC50 of 27 nM.
NMS-0963 displays high selectivity within a panel of tested kinases.
NMS-0963 effectively inhibits Syk phosphorylation and downstream signaling mediators of the BCR in treated cells.
NMS-0963 shows low nanomolar antiproliferative activity on BaF3-TEL/SYK cell lines with >200-fold selectivity versus BaF3-TEL/SYK cell lines + IL3.
NMS-0963 shows inhibitory activity in the diffuse large B cell lymphoma (DLBCL) cell line SUDHL-6 with IC50 of 702.4 nM.
NMS-0963 displays good pharmacokinetics properties, with linear exposure with dose and excellent oral bioavailability.
Physicochemical Properties
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M.Wt
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451.53
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Formula
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C23H29N7O3
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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(S)-N-(1-(azetidin-1-yl)propan-2-yl)-3-(2-((3,5-dimethoxyphenyl)amino)pyrimidin-4-yl)-1-methyl-1H-pyrazole-5-carboxamide
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References
1. Giovanni Cervi, et al. Eur J Med Chem. 2024 Apr 4:270:116375.
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