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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-Hec1/Nek2-NBI-961
NBI-961

Chemical Structure : NBI-961

CAS No.: 2225902-88-3

NBI-961 (NBI 961)

货号: PC-21395Not For Human Use, Lab Use Only.

NBI-961 is a highly potent, selective inhibitor of NIMA related Kinase 2 (NEK2) and FLT3 with IC50 of 32 nM and 37 nM, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

NBI-961 is a highly potent, selective inhibitor of NIMA related Kinase 2 (NEK2) and FLT3 with IC50 of 32 nM and 37 nM, respectively.
NBI-961 also shows inhibitory activities on FTL3-ITDD835V and FLT3-ITDF691L.
NBI-961 exhibits high binding affinity for NEK2 relative to >90 other kinases (scanEDGE® kinome panel, Eurofins DiscoverX), with exception for FLT3.
NBI-961 achieves growth inhibitory concentrations (GI50) in DLBCL cell in the nanomolar range.
NBI-961 leads to proteasomal degradation of NEK2 and is more effective than the indirect INH154 (Cat#PC-61480) NEK2 inhibitor in both DLBCL cell lines and patient derived cells.
NBI-961 sensitizes lymphoma cells to chemotherapy by inducing apoptosis.
NBI-961 (5 mg/kg, i.p., once-daily) delays DLBCL growth in vivo and prolongs survival of mouse models of DLBCL, with no visible signs of distress or toxicity including no visible weight loss and no loss of appetite, activity, or tuft fur.

物理化学性质&存储条件

分子量 568.62
分子式 C28H27F3N6O2S
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

5-[7-[1-[2-(Dimethylamino)ethyl]-1H-pyrazol-4-yl]imidazo[1,2-a]pyridin-3-yl]-3-[(1S)-1-[2-(trifluoromethyl)phenyl]ethoxy]-2-thiophenecarboxamide

参考文献

1. Mason McCrury, et al. Mol Cancer Ther. 2023 Oct 11. doi: 10.1158/1535-7163.MCT-23-0299.

2. Lingtian Zhang, et al. Eur J Med Chem. 2021 Dec 5:225:113776.

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