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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 |
| 5MG | 250 | In Stock |
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| 10MG | 398 | In Stock |
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| 25MG | 825 | In Stock |
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| 50MG | 1293 | In Stock |
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| 100MG | 2037 | In Stock |
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| 200MG | Get Quote | In Stock |
|
| 500MG | Get Quote | In Stock |
|
| 1G | Get Quote | In Stock |
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Biological Information
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Product NameSK-575
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NoteResearch use only, not for human use.
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Brief DescriptionSK-575 is a degradation agent targeting protein-hydrolyzed PARP1 chimera with anticancer and antitumor activity.
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DescriptionSK-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.
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In VitroWestern 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.
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In VivoAnimal 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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Synonyms——
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PathwayCell Cycle/DNA Damage
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TargetPARP
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RecptorPARP
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Research Area——
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Indication——
Chemical Information
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CAS Number2523016-96-6
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Formula Weight876.97
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Molecular FormulaC47H53FN8O8
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Purity>98% (HPLC)
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SolubilityIn Vitro:?DMSO : 100 mg/mL (114.03 mM; Ultrasonic )
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SMILESO=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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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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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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