AKI-001

• Target:

  Others

• Related Pathways:

  Others

• Bioactivity:

  AKI-001 is a potent Aurora kinase inhibitor, which exhibits low nanomolar potency against both Aurora A and Aurora B enzymes, excellent cellular potency (IC50 < 100 nM), and good oral bioavailability. Phenotypic cellular assays show that both Aurora A and Aurora B are inhibited at inhibitor concentrations sufficient to block proliferation. Importantly, the cellular activity translates to potent inhibition of tumor growth in vivo. An oral dose of 5 mg/kg QD is well tolerated and results in near stasis (92% TGI) in an HCT116 mouse xenograft model.

• Smiles:

  C (C) N1C=2C=C3C4=C (NC3=CC2C (C) (C) C1=O) C=5C (CCC4) =C (C) NN5

• Molecular Formula:

  C21H24N4O

• Molecular Weight:

  348.44

• Shipping Conditions:

  Cool pack

• Storage Temperature:

  -20°C

• CAS Number:

  925218-37-7