SK-575

SKU: orb1739884

Description

SK-575 is a small molecule degradation agent that selectively targets and degrades PARP1 chimera proteins. It demonstrates potent anticancer activity, particularly in BRCA1/2-mutant cancer cells, by inhibiting proliferation in vitro and showing efficacy in relevant tumor models in vivo.

Research Area

Epigenetics & Chromatin, Molecular Biology, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 2523016-96-6
• MW: 876.97
• Purity: 99.39%
• Formula: C₄₇H₅₃FN₈O₈
• SMILES: O=C1NN=C(C=2C=CC=CC12)CC3=CC=C(F)C(=C3)C(=O)N4CCN(C(=O)CCCCCCCCCCC(=O)NCCNC5=CC=CC=6C(=O)N(C(=O)C56)C7C(=O)NC(=O)CC7)CC4
• Target: PROTACs,PARP
• Solubility: DMSO:80 mg/mL (91.22 mM)

Bioactivity

• Target IC50:
  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)
• In Vivo:
  In male BALB/c nude mice bearing xenograft Capan-1 tumors, SK-575 (25 mg/kg, 50 mg/kg; intraperitoneal injection, once daily for 5 consecutive days) inhibited tumor growth. These doses of SK-575 (25 and 50 mg/kg) were well tolerated, with no observed mouse lethality or significant weight loss during the treatment period.
• In Vitro:
  In MDA-MB-436, Capan-1, and SW620 cells, SK-575 (10000, 1000, 300, 100, 30, 10, 3, 1, 0.3, 0.1, 0.03, and 0.01 nM; 24 hours) exhibited significant PARP1 degradation activity, with IC50 values of 1.26, 6.72, and 0.509 nM, respectively.

Storage & Handling

• Storage: keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

SK 575, SK575, SK-575, PARP1

Compound Identifiers

PubChem CID

162664494