SK-575 is a highly potent and specific proteolysis-targeting chimera (PROTAC) degrader of PARP1, with an IC 50 of 2.30 nM. SK-575 potently inhibits the growth of cancer cells bearing BRCA1/2 mutations.
性状
Solid
IC50 & Target[1][2]
PARP1 2.30 nM (IC50)
体外研究(In Vitro)
SK-575 抑制 MDA-MB-436 和 Capan-1 细胞生长,IC50 值分别为 19±6 nM 和 56±12 nM。SK-575 (0-1 μM,24 h) 在癌细胞系 (MDA-MB-436、Capan-1 和 SW620 细胞)中显示出良好的 PARP1 降解活性。SK-575 (0-10 μM, 24 h) 诱导 MDA-MB-436 和 Capan-1 细胞生成 γH2AX,呈剂量依赖性。 has not independently confirmed the accuracy of these methods. They are for reference only.Western Blot AnalysisM
体内研究(In Vivo)
SK-575 (25 和 50 mg/kg,腹腔注射,每天一次,持续 5 天) 在 HR 缺陷异种移植模型中作为单一药物显著抑制体内肿瘤生长。
SK-575 (25 mg/kg,腹腔注射,单次)在血浆中充分暴露超过 24 小时,并有效诱导 SW620 异种移植肿瘤组织中的 PARP1 降解,效果持续 >24 小时。 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
-20°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
参考文献
[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.
溶解度数据
In Vitro: DMSO : 100 mg/mL (114.03 mM; Need ultrasonic)配制储备液