InformationLY3295668 (AK-01) is a potent, orally active and specific inhibitor ofAurora A kinasewith Ki of 0.8 nM and 1038 nM for AURKA and AURKB, respectively.TargetsAURKA (Cell-free assay) 0.8 nM(Ki)In vitroLY3295668, an AURKA inhibitor with over 1,000-fold selectivity versus AURKB, is distinguished by minimal toxicity to bone marrow cells at concentrations active against RB1mut cancer cells.In vivoLY3295668 leads to durable regression of RB1mut tumor xenografts at exposures that are well tolerated in rodents. Genetic suppression screens identifi ed enforcers of the spindle-assembly checkpoint (SAC) as essential for LY3295668 cytotoxicity in RB1-defi cient cancers and suggest a model in which a primed SAC creates a unique dependency on AURKA for mitotic exit and survival.Cell Research(from reference)Cell lines：NCI-H446 cells, Calu-6 cells Concentrations：0.001 μM - 1 μM Incubation Time：24 h, 48 h, 72 h
Specifictaions: Moligand™, ≥99%
MDL Number: C24H26ClF2N5O2
Molecular Formula: 489.95
PubChem CID: 121333423
Isomeric SMILES: C[C@@H]1C[C@](CCN1CC2=C(C(=CC=C2)Cl)F)(CC3=C(C=CC(=N3)NC4=NNC(=C4)C)F)C(=O)O
- UPC:
- 42142303
- Condition:
- New
- Availability:
- 4-8 weeks
- Weight:
- 1.06 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- L414177-100mg
- CAS:
- 1919888-06-4
- Product Size:
- 100mg
