| Description | SK-575 is a degradation agent targeting protein-hydrolyzed PARP1 chimera with anticancer and antitumor activity.SK-575 effectively inhibits the growth of cancer cells harboring BRCA1/2 mutations and selectively induces PARP1 degradation in cancer cells. |
| In vitro | 在 MDA-MB-436、Capan-1 和 SW620 细胞中，SK-575（10000、1000、300、100、30、10、3、1、0.3、0.1、0.03和 0.01 nM；24小时）表现出良好的 PARP1降解活性，其 IC50 值分别为1.26、6.72 和0.509 nM[1]。 |
| In vivo | 在携带异种移植 Capan-1 肿瘤的雄性 BALB/c 裸鼠中，SK-575（25 mg/kg，50 mg/kg；腹腔注射，连续 5 天，每天 1 次）能够抑制肿瘤生长。这些剂量（25和 50 mg/kg）的 SK-575 耐受性良好，在治疗期间未观察到小鼠死亡或明显体重减轻[1]。 |
| Target activity | PARP1 degradation activity:6.72 nM (in Capan-1 cells), PARP1 degradation activity:1.26 nM (in MDA-MB-436 cells), PARP1 degradation activity:0.509 nM (in SW620 cells) |
| molecular weight | 876.97 |
| Molecular formula | C47H53FN8O8 |
| CAS | 2523016-96-6 |
| Storage | keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 80 mg/mL (91.22 mM), Sonication is recommended. |
| References | 1. Cao C, et al. Discovery of SK-575 as a Highly Potent and Efficacious Proteolysis-Targeting Chimera Degrader of PARP1 for Treating Cancers. J Med Chem. 2020 Oct 8;63(19):11012-11033. |