| Identification | Back Directory | [Name]
Spiro[3H-indole-3,4'-piperidin]-2(1H)-one, 6-[(2R,6S)-2,6-dimethyl-4-morpholinyl]-4-fluoro-1'-(3,4,5,6,7,8-hexahydro-8-methyl-4-oxopyrido[2,3-d]pyrimidin-2-yl)-1-methyl-, rel- | [CAS]
2171388-28-4 | [Synonyms]
Spiro[3H-indole-3,4'-piperidin]-2(1H)-one, 6-[(2R,6S)-2,6-dimethyl-4-morpholinyl]-4-fluoro-1'-(3,4,5,6,7,8-hexahydro-8-methyl-4-oxopyrido[2,3-d]pyrimidin-2-yl)-1-methyl-, rel- | [Molecular Formula]
C27H35FN6O3 | [MOL File]
2171388-28-4.mol | [Molecular Weight]
510.6 |
| Hazard Information | Back Directory | [Description]
RK-582 is an orally efficacious spiroindolinone-based tankyrase inhibitor for the treatment of colon cancer. It exhibits a markedly improved robust tumor growth inhibition in a COLO-320DM mouse xenograft model when orally administered. | [Uses]
RK-582 is an orally active, spiroindoline-based selective inhibitor of tankyrase. The IC50s of RK-582 against TNKS1/PARP5A and PARP1 are 36.1 nM and 18.168 nM, respectively. RK-582 inhibits rectal cancer COLO-320DM cells (GI50=0.23 μM) and significantly inhibits tumor growth in a COLO-320DM mouse xenograft model[1]. | [References]
[1] Shirai F et al. Design and Discovery of an Orally Efficacious Spiroindolinone-Based Tankyrase Inhibitor for the Treatment of Colon Cancer. J Med Chem. 2020 Apr 23;63(8):4183-4204. DOI:10.1021/acs.jmedchem.0c00045 |
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