| Description | CX-6258 hydrochloride (Pim-Kinase Inhibitor X) is an effective, orally efficacious Pim1/2/3 kinase inhibitor (IC50: 5/25/16 nM). |
| In vitro | CX-6258 has anti-proliferative activity against a panel of human cancer cell lines (IC50: 0.02-3.7 μM), mostly sensitive to acute leukemia cell lines. Combinations of CX-6258 with doxorubicin (10:1 molar ratio) and CX-6258 with paclitaxel (100:1 molar ratio) produces synergistic cell killing (CI50: 0.4 and 0.56). |
| In vivo | In mice carrying MV-4-11 xenografts, CX-6258 dose-dependently suppresses the tumor growth , with a 50/100 mg/kg dose producing 45%/75% tumor growth inhibition. |
| Target activity | Pim1:5 nM, Pim3:16 nM, Pim2:25 nM |
| Synonyms | CX-6258 HCl, Pim-Kinase Inhibitor X |
| molecular weight | 498.4 |
| Molecular formula | C26H24ClN3O3·HCl |
| CAS | 1353859-00-3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | H2O: 82 mg/mL (164.5 mM) DMSO: 53 mg/mL (106.3 mM) Ethanol: 1 mg/mL (2.0 mM), Heating is recommended. |
| References | 1. Haddach M, et al. ACS Medicinal Chemistry Letters, 3 (2) , 135-139 |