SK-575

Research use only, not for human use.

SK-575 is a degradation agent targeting protein-hydrolyzed PARP1 chimera with anticancer and antitumor activity.

SK-575 is a highly potent and specific proteolysis-targeting chimera (PROTAC) degrader of PARP1, with an IC50 of 2.30 nM. SK-575 potently inhibits the growth of cancer cells bearing BRCA1/2 mutations.

Western Blot AnalysisMCell Line:MDA-MB-436, Capan-1, and SW620 cells Concentration:10000, 1000, 300, 100, 30, 10, 3, 1, 0.3, 0.1, 0.03, and 0.01 nM Incubation Time:24 h Result:Showed good PARP1 degradation activity in these cancer cell lines (MDA-MB-436, Capan-1, and SW620 cells), with IC50 values of 1.26, 6.72 and 0.509 nM, respectively. Effectively induced the formation of γH2AX in MDA-MB-436 and Capan-1 cells in a dose dependent manner.

Animal Model:Male BALB/c nude mice (bearing xenograft Capan-1 tumors)Dosage:25 mg/kg, 50 mg/kg Administration:IP, once daily for 5 consecutive days Result:Inhibited tumor growth. SK-575 at these doses (25 and 50 mg/kg) were well tolerated, with no mice lethality or significant weight loss observed during the treatment time.Animal Model:Female ICR mice (20-23 g, 6-7 week-old, n=3 per group) Dosage:25 mg/kg Administration: Intraperitoneally, a single dose (Pharmacokinetic Analysis)Result:Pharmacokinetic Parameters of SK-575 in female ICR mice.

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Cell Cycle/DNA Damage

PARP

PARP

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2523016-96-6

876.97

C47H53FN8O8

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (114.03 mM; Ultrasonic )

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

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(-20℃)

With Ice Pack

≥ 2 years