Chemical Structure : AM-9022
CAS No.:
2446872-46-2
AM-9022
(AM9022)
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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578.68
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Formula
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C27H36F2N6O4S
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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(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
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References
1. Marc Payton, et al. Nat Cancer. 2023 Dec 27. doi: 10.1038/s43018-023-00699-5.
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