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首页-小分子抑制剂&激动剂-Cytoskeleton/Cell Adhesion Molecules-Kinesin-AM-1882
AM-1882

Chemical Structure : AM-1882

CAS No.: 2600559-12-2

AM-1882 (AM1882)

货号: PC-21659Not For Human Use, Lab Use Only.

AM-1882 (AM1882) is a potent, selective mitotic kinesin KIF18A inhibitor with IC50 of 230 nM in kinesin-8 microtubule (MT)-ATPase motor assays.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

AM-1882 (AM1882) is a potent, selective mitotic kinesin KIF18A inhibitor with IC50 of 230 nM in kinesin-8 microtubule (MT)-ATPase motor assays.
AM-1882 exhibits good specificity against a panel of diverse kinesin motor proteins, except for the KIF19A motor (IC50=1820 nM).
AM-1882 shows cellular EC50 of 21 and 15 nM for cell line pH3+ and PCM foci in mitotic image assays respectively.
AM-1882 has similar inhibitory effects on the motor activity of human and mouse KIF18A.
AM-1882 is active in a subset of cancer cell lines with CCNE1, BRCA1 and RB1 gene alterations and can enhance apoptosis when combined with PARP inhibition.
AM-1882 (50 or 100 mg per kg, i.p.) inhibited tumor growth in OVCAR-8 CDX tumor model.

物理化学性质&存储条件

分子量 576.77
分子式 C28H40N4O5S2
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

4-(N-(tert-butyl)sulfamoyl)-N-(3-(N-(tert-butyl)sulfamoyl)phenyl)-2-(6-azaspiro[2.5]octan-6-yl)benzamide

参考文献

1. Marc Payton, et al. Nat Cancer. 2023 Dec 27. doi: 10.1038/s43018-023-00699-5.

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