Chemical Structure : NMS-0963
货号: 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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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.
分子量 | 451.53 | |
分子式 | C23H29N7O3 | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
1. Giovanni Cervi, et al. Eur J Med Chem. 2024 Apr 4:270:116375.
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