CDK2/PIM1-IN-1
CDK2/PIM1-IN-1 is an inhibitor of CDK2 (IC50: 0.27 μM) and PIM1 (IC50: 0.67 μM) kinases. CDK2/PIM1-IN-1 induces apoptosis and reduces tumor-promoting TNF-α expression. CDK2/PIM1-IN-1 has antitumor activity.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Formule: C27H23N3O2
- Masse moléculaire:421.49
-
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]|
CDK2 0.27 μM (IC50) |
PIM1 0.67 μM (IC50) |
In Vitro
CDK2/PIM1-IN-1 (Compound 6b) (24 h) shows antiproliferative effects on MCF7 cells (IC50: 5.54 μM), HCT-116 cells (IC50: 2.62 μM), HepG2 cells (IC50: 3.99 μM) and HeLa cell lines (IC50: 8.31 μM), with moderate safety in the normal breast cell line MCF-10A (IC50: 39.44 μM) [1].
CDK2/PIM1-IN-1 (24 h) inhibits HCT116 cell line at the G0-G1 phase (%G0-G1: 83.43%) and induced significant early (8.28%) and late (20.09%) cell apoptosis[1].
CDK2/PIM1-IN-1 (24 h) shows inhibitory effects on both CDK (IC50: 0.27 μM) and PIM1 (IC50: 0.67 μM) in HCT116 cell lines[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:Tumor cell line (MCF7 cells, HCT-116 cells, HepG2 cells, HeLa cell lines), and the normal breast cell line MCF-10A.
-
Concentration:
-
Incubation Time:24 h
-
Result:Inhibited the cell viability of MCF7 cells (IC50: 5.54 μM), HCT-116 cells (IC50: 2.62 μM), HepG2 cells (IC50: 3.99 μM) and HeLa cell lines (IC50: 8.31 μM).
Showed moderate safety in the normal breast cell line MCF-10A (IC50: 39.44 μM).
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Solid Ehrlich carcinoma (SEC) mouse model[1]
-
Dosage:10 mg/kg
-
Administration:Intraperitoneal injection (i.p.), three times weekly for two weeks.
-
Result:Reduced tumor volume (71.42%) and weight (70.58%).
Showed good tolerability (indicated by stable body weight and 100% survival rate compared with the Dox-treated group).
Inhibited CDK2 (70.96%) and PIM1 (53.61%) levels in mouse tumors, tumor cell mitosis (27.35%).
Inhibited tumor TNF-α expression (17.61%).
Chemical Information
-
Masse moléculaire 421.49
-
Formule C27H23N3O2
-
SMILES
COC1=CC=C(C2=CC=NC3=C2C(C4=CC=C(C)C=C4)=NN3C5=CC=CC=C5)C=C1OC
-
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)
CDK2/PIM1-IN-1 Related Classifications
HY-173224 Related Classifications
Powered by Bioz