Pim-1 kinase inhibitor 8
Based on 1 Customer Validation
Pim-1 kinase inhibitor 8 is a potent PIM-1 inhibitor with an IC50 value of 14.3 nM. Pim-1 kinase inhibitor 8 impedes cell proliferation and migration through PIM-1 inhibition and the induction of both apoptosis and autophagy. Pim-1 kinase inhibitor 8 inhibits solid tumor growth in Solid Ehrlich Carcinoma (SEC)-bearing mice. Pim-1 kinase inhibitor 8 can be used for breast and liver cancer research.
For research use only. We do not sell to patients.
- Purity: 99.90%
- CAS No.: 916038-47-6
- Formula: C14H17N3O3
- Molecular Weight:275.30
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
Pim-1 kinase inhibitor 8 (compound 12) (0.01-100 μM, 48 h) exhibits potent cytotoxicity against MCF-7 and HepG2 cell lines with IC50 values of 0.51 μM and 5.27 μM, respectively, while showing much lower potency in normal MCF-10A cells (IC50 = 52.85 μM)[1].
Pim-1 kinase inhibitor 8 (1.62 μM, 48 h) triggers considerable apoptotic and autophagic cell death in MCF-7 cells, accompanied by cell cycle arrest at the S-phase, and shows significant inhibition of cell migration (71.8 % wound closure vs. 95.6 % in the control)[1].
Pim-1 kinase inhibitor 8 binds strongly to the PIM-1 active site (-17.38 kcal/mol) by forming a key hydrogen bond with Lys67 and multiple hydrophobic interactions[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:MCF-7 cells
-
Concentration:1.62 μM
-
Incubation Time:48 h
-
Result:Increased the proportion of cells in the S-phase to 36.02%, compared to 29.12% in the control.
Reduced the proportion of cells in the G2/M phase from 16.05% (control) to 7.56%.
-
Cell Line:MCF-7 cells
-
Concentration:1.62 μM
-
Incubation Time:48 h
-
Result:Increased total apoptosis by 33.43% (23.18% for early apoptosis and 10.25% for late apoptosis) compared to the untreated control group (0.64%).
Increased apoptosis by 52.2-fold.
-
Cell Line:MCF-7 and HepG2 cells
-
Concentration:0.01, 0.1, 1, 10, and 100 μM
-
Incubation Time:48 h
-
Result:Inhibited the growth of MCF-7 and HepG2 cells by 84.20% and 85.13%, respectively, at 100 μM.
-
Cell Line:MCF-7 cells
-
Concentration:1.62 μM
-
Incubation Time:48 h
-
Result:Caused considerable autophagic cell death, markedly increasing the autophagic cell population to 87.6 × 103 cells compared to 32.8 × 103 in the control.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Adult female Swiss albino mice (18-23 g) subcutaneously injected with SEC cells[1]
-
Dosage:5 mg/kg
-
Administration:i.p., daily for 24 days
-
Result:Decreased tumor weight from 198.5 mg in control to 72.8 mg.
Reduced tumor volume from 274.8 mm3 in the untreated control to 159.2 mm3.
Greatly decreased tumor proliferation by 42.1%.
Chemical Information
-
CAS No. 916038-47-6
-
Appearance Solid
-
Molecular Weight 275.30
-
Formula C14H17N3O3
-
Color White to off-white
-
SMILES
N#CC1=C(OCC(N2CCOCC2)=O)N=C(C)C=C1C
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 125 mg/mL (454.05 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
-
Data Sheet (277 KB)
-
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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. 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 | 3.6324 mL | 18.1620 mL | 36.3240 mL | 90.8100 mL |
| 5 mM | 0.7265 mL | 3.6324 mL | 7.2648 mL | 18.1620 mL | |
| 10 mM | 0.3632 mL | 1.8162 mL | 3.6324 mL | 9.0810 mL | |
| 15 mM | 0.2422 mL | 1.2108 mL | 2.4216 mL | 6.0540 mL | |
| 20 mM | 0.1816 mL | 0.9081 mL | 1.8162 mL | 4.5405 mL | |
| 25 mM | 0.1453 mL | 0.7265 mL | 1.4530 mL | 3.6324 mL | |
| 30 mM | 0.1211 mL | 0.6054 mL | 1.2108 mL | 3.0270 mL | |
| 40 mM | 0.0908 mL | 0.4541 mL | 0.9081 mL | 2.2703 mL | |
| 50 mM | 0.0726 mL | 0.3632 mL | 0.7265 mL | 1.8162 mL | |
| 60 mM | 0.0605 mL | 0.3027 mL | 0.6054 mL | 1.5135 mL | |
| 80 mM | 0.0454 mL | 0.2270 mL | 0.4541 mL | 1.1351 mL | |
| 100 mM | 0.0363 mL | 0.1816 mL | 0.3632 mL | 0.9081 mL |
Pim-1 kinase inhibitor 8 Related Classifications
HY-162006 Related Classifications
Powered by Bioz