| 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].
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| Related Catalog |
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| Target |
PARP1
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| 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].
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| 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.
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