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

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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Customer Review

Based on 1 publication(s) in Google Scholar

SK-575 Related Antibodies

Top Publications Citing Use of Products

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  • Biological Activity

  • Purity & Documentation

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  • Customer Review

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)

Cellular Effect
Cell Line Type Value Description References
CAPAN-1 IC50
0.056 μM
Compound: 18; SK-575
Antiproliferative activity against human CAPAN-1 cells assessed as cell growth inhibition incubated for 13 days by by CCK-8 assay
Antiproliferative activity against human CAPAN-1 cells assessed as cell growth inhibition incubated for 13 days by by CCK-8 assay
[PMID: 32924477]
MDA-MB-436 IC50
0.019 μM
Compound: 18; SK-575
Antiproliferative activity against human MDA-MB-436 cells assessed as cell growth inhibition incubated for 7 days by CCK-8 assay
Antiproliferative activity against human MDA-MB-436 cells assessed as cell growth inhibition incubated for 7 days by CCK-8 assay
[PMID: 32924477]
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].

MedChemExpress (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 DC50 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].

MedChemExpress (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

Formula

C47H53FN8O8
CAS No.
Appearance

Solid

Color

Light yellow to yellow

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; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

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C1

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Volume (start)

V1

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Concentration (final)

C2

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Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.51%

SDS (252 KB)

COA (243 KB) HNMR (376 KB) LCMS (126 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.1403 mL 5.7014 mL 11.4029 mL 28.5072 mL
5 mM 0.2281 mL 1.1403 mL 2.2806 mL 5.7014 mL
10 mM 0.1140 mL 0.5701 mL 1.1403 mL 2.8507 mL
15 mM 0.0760 mL 0.3801 mL 0.7602 mL 1.9005 mL
20 mM 0.0570 mL 0.2851 mL 0.5701 mL 1.4254 mL
25 mM 0.0456 mL 0.2281 mL 0.4561 mL 1.1403 mL
30 mM 0.0380 mL 0.1900 mL 0.3801 mL 0.9502 mL
40 mM 0.0285 mL 0.1425 mL 0.2851 mL 0.7127 mL
50 mM 0.0228 mL 0.1140 mL 0.2281 mL 0.5701 mL
60 mM 0.0190 mL 0.0950 mL 0.1900 mL 0.4751 mL
80 mM 0.0143 mL 0.0713 mL 0.1425 mL 0.3563 mL
100 mM 0.0114 mL 0.0570 mL 0.1140 mL 0.2851 mL
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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.

Keywords:

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

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