PLK1-IN-16
PLK1-IN-16 is a selective polo-like kinase 1 (PLK1) inhibitor with an IC50 of 0.25 nM. PLK1-IN-16 exhibits lower inhibitory potency against PLK2 and PLK3, induces G2 phase cell cycle arrest, induces apoptosis, and exhibits antiproliferative activity against tumor cells. PLK1-IN-16 can be stable under simulated gastric acid environmental conditions, and acceptable CYP 450 inhibition. PLK1-IN-16 can be used for the study of triple-negative breast cancer (TNBC), breast cancer, leukemia.
Para uso exclusivo en investigación. No vendemos a pacientes.
- No. CAS: 3068378-51-5
- Fòrmula: C26H34N6O4S
- Peso molecular:526.65
-
Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Actividad biológica
-
Chemical Information
- Pureza y Documentación
- Referencias
-
Help & FAQs
Actividad biológica
Descripciòn
IC50 & Target
[1]|
PLK1 0.25 nM (IC50) |
PLK2 15.7 nM (IC50) |
PLK3 8.97 nM (IC50) |
In Vitro
PLK1-IN-16 (compound B7) inhibits proliferation of MDA-MB-231, MDA-MB-361, and MV-4-11 cells with IC50 values of 72.5 nM, 316 nM, and 32.1 nM respectively[1].
PLK1-IN-16 (12.5-200 nM; 72 h) arrests MV-4-11 cells in the G2 phase in a dose-dependent manner[1].
PLK1-IN-16 (5.0-80.0 nM; 72 h) induces apoptosis in MV-4-11 cells in a dose-dependent manner[1].
PLK1-IN-16 (2 h) is stable under simulated gastric acid conditions with a residual rate of 98.4% after 2 h[1].
PLK1-IN-16 has weak inhibitory effects on CYP1A2, CYP2C9, CYP2C19, and CYP2D6, and strong inhibition of CYP3A4 (IC50 of ~1 μM)[1].
PLK1-IN-16 has high plasma protein binding rates in human (99.6%), rat (99.7%), and mouse (99.4%) plasma[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:MV-4-11
-
Concentration:12.5 nM,
25.0 nM, 50.0 nM, 100 nM, and 200 nM -
Incubation Time:72 h
-
Result:Induced G2 phase arrest in a dose-dependent manner, with 4N DNA aggregation observed starting at 100 nM.
-
Cell Line:MV-4-11
-
Concentration:5.0 nM,
10.0 nM, 20.0 nM, 40.0 nM and 80.0 nM -
Incubation Time:72 h
-
Result:Increased apoptosis rate in a concentration-dependent manner, with rates ranging from 10.98% to 34.09%.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
No. CAS 3068378-51-5
-
Peso molecular 526.65
-
Fòrmula C26H34N6O4S
-
SMILES
O=S(N1C2=CC(OC)=C(NC3=NC=C4C(N(C5CCCC5)[C@H](CC)C(N4C)=O)=N3)C=C2CC1)(C6CC6)=O
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PLK1-IN-16 Related Classifications
HY-181051 Related Classifications
Powered by Bioz