PLK1-IN-12
PLK1-IN-12 is a highly selective and orally active PLK1 inhibitor with an IC50 of 20 nM. PLK1-IN-12 shows more selective for PLK1 than PLK2 (IC50: >10000 nM) and PLK3 (IC50: 3953 nM). PLK1-IN-12 exhibits anticancer potency across a broad spectrum of cell lines. PLK1-IN-12 can be used in anti-leukemia research.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Formule: C28H40ClN7O3
- Masse moléculaire:558.12
-
Stockage:
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]
-
Activité biologique
-
Chemical Information
- Pureté et documentation
- Références
-
Help & FAQs
Activité biologique
Description
IC50 & Target
[1]|
PLK1 20 nM (IC50) |
PLK2 >10000 nM (IC50) |
PLK3 3953 nM (IC50) |
In Vitro
PLK1-IN-12 (Compound B31) (0.508 nM-10 μM, 24 h) shows antiproliferative effects in H460 (IC50: 12 nM), A549 (IC50: 32 nM), SW620 (IC50: 8.2 nM), HL-60 (IC50: 59 nM), K562 (IC50: 0.08 nM) and CCRF-CEM (IC50: 41 nM) cell lines[1].
PLK1-IN-12 (1 μM, 5 min) shows rapid clearance in human, mouse and dog liver microsomes (Clint: 68.3-210 μL/min/mg protein)[1].
PLK1-IN-12 (0.1-30 μM, 24 h) has a low inhibitory effect on HEK293T cells viability (68%)[1].
PLK1-IN-12 (0.4-100 μM) has a low inhibitory effect on hERG potassium channels (IC50: 44.2 μM), indicating a low risk of cardiotoxicity[1].
PLK1-IN-12 (10 μM, 5-30 min) has no inhibitory effect on CYP1A2, CYP3A4, CYP2D6, CYP2B6 and CYP2C8, and only has weak inhibitory effects on CYP2C9 and CYP2C19, indicating that it is stable in both human and rat hepatocytes and has a low possibility of drug interactions[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:H460、PC-9、A549、SW620、HL-60、K562、CCRF-CEM and KG-1 cell lines
-
Concentration:1.00 × 10-5, 3.33 × 10-6, 1.11 × 10-6, 3.7 × 10-7, 1.23 × 10-7, 4.12 × 10-8, 1.37 × 10-8, 4.57 × 10-9, 1.52 × 10-9, and 5.08 × 10-10 mol/L
-
Incubation Time:24 h
-
Result:Showed antiproliferative effects in H460 (IC50: 12 nM), A549 (IC50: 32 nM), SW620 (IC50: 8.2 nM), HL-60 (IC50: 59 nM), K562 (IC50: 0.08 nM) and CCRF-CEM (IC50: 41 nM) cell lines.
-
Cell Line:HEK293T cells
-
Concentration:0.1, 0.3, 1, 3, 10, and 30 μM
-
Incubation Time:24 h
-
Result:Had a low inhibitory effect on cell viability of HEK293T cells (68%).
Parmacokinetics
In Vivo
PLK1-IN-12 (500 mg/kg, i.g., once daily for 7 d) has no tissue damage or toxicity to various organs of mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Subcutaneous K562 cell transplantation tumor model, Male BALB/c mice (6–8 weeks old, weighing 18–20 g)[1]
-
Dosage:10/20 mg/kg
-
Administration:Intragastric (i.g.), twice weekly for 11 d
-
Result:Inhibited tumor growth.
-
Animal Model:Acute toxicity test[1]
-
Dosage:500 mg/kg
-
Administration:Intragastric (i.g.), once daily for 7 d
-
Result:Compared with the mice in the positive control group, there was no significant change in body weight, and no obvious damage to the heart, kidney, lung, liver and spleen.
Chemical Information
-
Masse moléculaire 558.12
-
Formule C28H40ClN7O3
-
SMILES
CN(C1=O)C(C=NC(NC2=C(C(Cl)=CC(N3CCN(CC3)C)=C2)OCCCO)=N4)=C4N([C@@H]1CC)C5CCCC5
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PLK1-IN-12 Related Classifications
HY-172364 Related Classifications
Powered by Bioz