2. Cell Cycle/DNA Damage Epigenetics PROTAC
  3. PARP PROTACs
  4. SK-575

SK-575 

Cat. No.: HY-139156 Purity: 99.51%
COA Handling Instructions

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.

For research use only. We do not sell to patients.

SK-575 Chemical Structure

SK-575 Chemical Structure

CAS No. : 2523016-96-6

Size Price Stock Quantity
5 mg USD 320 In-stock
10 mg USD 510 In-stock
25 mg USD 1050 In-stock
50 mg USD 1680 In-stock
100 mg USD 2650 In-stock
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500 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

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  • Biological Activity

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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[1].

IC50 & Target

PARP1

2.30 nM (IC50)

In Vitro

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].
SK-575 (0-1 μM, 24 h) shows good PARP1 degradation activity in cancer cell lines (MDA-MB-436, Capan-1, and SW620 cells)[1].
SK-575 (0-10 μM, 24 h) effectively induces the formation of γH2AX in MDA-MB-436 and Capan-1 cells in a dose dependent manner[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

SK-575 Related Antibodies

Western Blot AnalysisM[1]

Cell 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

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].
SK-575 (25 mg/kg, IP, once) 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male BALB/c nude mice (bearing xenograft Capan-1 tumors)[1]
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)[1]
Dosage: 25 mg/kg
Administration: Intraperitoneally, a single dose (Pharmacokinetic Analysis)
Result: Pharmacokinetic Parameters of SK-575 in female ICR mice[1].
Parameters mean
Tmax (h) 0.25
Cmax (ng/mL) 1843
AUCall (ng/mL∗h) 5316
AUCinf (ng/mL∗h) 5363
t1/2 (ng/mL) 3.08
Molecular Weight

876.97

Appearance

Solid

Formula

C47H53FN8O8
CAS No.
SMILES

O=C(NCCNC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O)CCCCCCCCCCC(N4CCN(C(C5=CC(CC6=NNC(C7=C6C=CC=C7)=O)=CC=C5F)=O)CC4)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (114.03 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.1403 mL 5.7014 mL 11.4029 mL
5 mM 0.2281 mL 1.1403 mL 2.2806 mL
10 mM 0.1140 mL 0.5701 mL 1.1403 mL
*Please refer to the solubility information to select the appropriate solvent.
Purity & Documentation

Purity: 99.51%

COA (244 KB) HNMR (376 KB) LCMS (126 KB)

Handling Instructions (2659 KB)
References
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SK-575 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

SK-5752523016-96-6SK575SK 575PARPPROTACspoly ADP ribose polymeraseMDA-MB-436Capan-1 cellsPROTACanticancerSW620 cellsInhibitorinhibitorinhibit

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