Reactivos e instrumentos para inmunología, biología celular y biología molecular.
 
> SK-575 [2523016-96-6]

SK-575 [2523016-96-6]

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Referencia HY-139156-5mg

embalaje : 5mg

Marca : MedChemExpress


Descripciòn

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
Peso molecular

876.97

Fòrmula

C47H53FN8O8
No. CAS
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
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

-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)

Solvente y solubilidad
In Vitro: 

DMSO : 80 mg/mL (91.22 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.

  • Calculadora de molaridad

  • Calculadora de dilución

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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
Pureza y Documentación
Referencias

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