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首页-小分子抑制剂&激动剂-Tyrosine Kinase-Syk-NMS-0963
NMS-0963

Chemical Structure : NMS-0963

CAS No.: 2765304-82-1

NMS-0963 (NMS0963)

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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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

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.

物理化学性质&存储条件

分子量 451.53
分子式 C23H29N7O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(S)-N-(1-(azetidin-1-yl)propan-2-yl)-3-(2-((3,5-dimethoxyphenyl)amino)pyrimidin-4-yl)-1-methyl-1H-pyrazole-5-carboxamide

参考文献

1. Giovanni Cervi, et al. Eur J Med Chem. 2024 Apr 4:270:116375.

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