SK-575

Names

[ Name ]:
SK-575

Biological Activity

[Description]:

SK-575 is a highly potent and specific proteolysis-targeting chimera (PROTAC) degrader of PARP1. SK-575 potently inhibits the growth of cancer cells bearing BRCA1/2 mutations. SK-575 inhibits cell growth in MDA-MB-436 and Capan-1 cells, with IC50 values of 19 ± 6 nM and 56 ± 12 nM, respectively[1].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Epigenetics >> PARP

Signaling Pathways >> PROTAC >> PROTAC

Signaling Pathways >> Cell Cycle/DNA Damage >> PARP

[Target]

PARP1

[In Vivo]

SK-575 achieves sufficient exposure in plasma for over 24 h and effectively induces PARP1 degradation in the SW620 xenograft tumor tissue with the effect persisting for >24 h[1]. SK-575 (mice bearing BRCA2-mutated Capan-1 xenografts, 25 and 50 mg/kg, IP, once daily for 5 days) significantly inhibits the tumor growth in vivo as a single-agent in HR-deficient xenograft models[1].

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₄₇H₅₃FN₈O₈

[ Molecular Weight ]:
876.97

SK-575

Names

Biological Activity

Chemical & Physical Properties

Related Compounds