| Bioactivity | 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]. |
| Target | IC50: 36.1 nM (TNKS1/PARP5A), 18.168 nM (PARP1) |
| Name | RK-582 |
| CAS | 2171388-28-4 |
| Formula | C27H35FN6O3 |
| Molar Mass | 510.60 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. |