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Description: Potent and selective KIF18A inhibitor
Chemical Name: 2-(6-Azaspiro[2.5]oct-6-yl)-N-[2-(4,4-difluoro-1-piperidinyl)-6-methyl-4-pyrimidinyl]-4-[[[(1R)-2-hydroxy-1-methylethyl]sulfonyl]amino]benzamide
Purity: ≥98% (HPLC)
Biological Activity for AM 9022
AM 9022 is a potent and selective KIF18A inhibitor (IC50 = 60 nM). It displays selectivity for KIF18A over a panel of diverse kinesin motor proteins. Upon blocking MT-ATPase motor activity (non-competitive with ATP and MTs), it activates the mitotic checkpoint and selectively kills chromosomally unstable cancer cells. Has minimal detrimental effects on human bone marrow cells in culture, distinct from other anti-mitotic agents. In mice, inhibition of KIF18A leads to robust anti-cancer effects with tumor regression observed in human HGSOC and TNBC models at well-tolerated doses. AM 9022 can be used for the selective targeting of CIN cancers.
Technical Data for AM 9022
| M. Wt | 578.68 |
| Formula | C27H36F2N6O4S |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 2446872-46-2 |
| PubChem ID | 148785380 |
| InChI Key | OLCRYQGHHMGOJZ-LJQANCHMSA-N |
| Smiles | CC1=CC(NC(C2=C(C=C(C=C2)NS([C@H](C)CO)(=O)=O)N3CCC4(CC3)CC4)=O)=NC(N5CCC(F)(CC5)F)=N1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for AM 9022
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 57.87 | 100 |
Preparing Stock Solutions for AM 9022
The following data is based on the product molecular weight 578.68. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.73 mL | 8.64 mL | 17.28 mL |
| 5 mM | 0.35 mL | 1.73 mL | 3.46 mL |
| 10 mM | 0.17 mL | 0.86 mL | 1.73 mL |
| 50 mM | 0.03 mL | 0.17 mL | 0.35 mL |
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Product Datasheets for AM 9022
References for AM 9022
References are publications that support the biological activity of the product.
Payton et al (2023) Small-molecule inhibition of kinesin KIF18A reveals a mitotic vulnerability enriched in chromosomally unstable cancers. Nature Cancer 5 66 PMID: 38151625
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Cell Cycle and DNA Damage Research Product Guide
This product guide provides a review of the cell cycle and DNA damage research area and lists over 150 products, including research tools for:
- Cell Cycle and Mitosis
- DNA Damage Repair
- Targeted Protein Degradation
- Ubiquitin Proteasome Pathway
- Chemotherapy Targets
Cell Cycle & DNA Damage Repair Poster
In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. This poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.