SK-575

CAS No. 2523016-96-6

SK-575( —— )

Catalog No. M36290 CAS No. 2523016-96-6

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

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
2MG 163 Get Quote
5MG 250 Get Quote
10MG 398 Get Quote
25MG 799 Get Quote
50MG 1279 Get Quote
100MG 1971 Get Quote
500MG Get Quote Get Quote
1G Get Quote Get Quote

Biological Information

  • Product Name
    SK-575
  • Note
    Research use only, not for human use.
  • Brief Description
    SK-575 is a degradation agent targeting protein-hydrolyzed PARP1 chimera with anticancer and antitumor activity.
  • Description
    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.
  • In Vitro
    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.
  • In Vivo
    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.
  • Synonyms
    ——
  • Pathway
    Cell Cycle/DNA Damage
  • Target
    PARP
  • Recptor
    PARP
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    2523016-96-6
  • Formula Weight
    876.97
  • Molecular Formula
    C47H53FN8O8
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 100 mg/mL (114.03 mM; Ultrasonic )
  • 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
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

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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