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.
CAS 925218-37-7 MFCD025218377
化学结构图
SMILES: CCN1C(=O)C(C)(C)c2cc3c(cc21)C1CCCC2C(C)=NN=C2C1=N3
化学属性
| Mol. Weight | 348.44146 |
|---|---|
| Appearance | Solid powder |
| Solubility | Soluble in DMSO, not in water |
别名和识别编码
| Chemical Name | 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. |
|---|---|
| Formula | C21H24N4O |
| Synonym | AK-I001; AKI 001; AKI001. |
| IUPAC Name | 8-ethyl-3,10,10-trimethyl-4,5,6,6a,8,10-hexahydropyrazolo[4',3':6,7]cyclohepta[1,2-b]pyrrolo[2,3-f]indol-9(3aH)-one |
| InChIKey | XJDJFAMUCGWJHO-UHFFFAOYSA-N |
| InChI | InChI=1S/C21H24N4O/c1-5-25-17-9-14-13-8-6-7-12-11(2)23-24-19(12)18(13)22-16(14)10-15(17)21(3,4)20(25)26/h9-10,12-13H,5-8H2,1-4H3 |
| Canonical SMILES | O=C1C(C)(C)C2=CC3=C(C=C2N1CC)C(CCCC4C5=NN=C4C)C5=N3 |
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- 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.
