AM-9022 | Kif18A inhibitor | Probechem Biochemicals

Chemical Structure : AM-9022

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AM-9022 (AM9022)

货号: PC-21658Not For Human Use, Lab Use Only.

AM-9022 (AM9022) is a potent, selective and orally active mitotic kinesin KIF18A inhibitor with IC50 of 47 nM in kinesin-8 microtubule (MT)-ATPase motor assays.

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生物&药学活性

AM-9022 (AM9022) is a potent, selective and orally active mitotic kinesin KIF18A inhibitor with IC50 of 47 nM in kinesin-8 microtubule (MT)-ATPase motor assays.
AM-9022 exhibits good specificity against a panel of diverse kinesin motor proteins, except for the KIF19A motor (IC50=926 nM).
AM-9022 shows cellular EC50 of 42 and 37 nM for cell line pH3+ and PCM foci in mitotic image assays respectively.
AM-9022 has similar inhibitory effects on the motor activity of human and mouse KIF18A.
AM-9022 (30 mg per kg, p.o.) increased pH3 mitotic marker levels in OVCAR-3 tumors by 3.4-fold in the OVCAR-3 HGSOC CDX tumor model, inhibited tumor growth with evidence of TR (95% TR) and no body weight loss.
AM-9022 administered at 30 and 100 mg per kg inhibited tumor growth with evidence of TR (16% and 94% TR, respectively) at well-tolerated doses in JIMT-1 breast cancer CDX tumor model.

物理化学性质&存储条件

分子量	578.68
分子式	C27H36F2N6O4S
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	(R)-N-(2-(4,4-difluoropiperidin-1-yl)-6-methylpyrimidin-4-yl)-4-((2-hydroxy-1-methylethyl)sulfonamido)-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.

AM-9022 (AM9022)

生物&药学活性

物理化学性质&存储条件

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AM-9022 (AM9022)

生物&药学活性

物理化学性质&存储条件

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