| Description | CX-6258 is an orally valid Pim 1/2/3 kinase(IC50=5 nM/25 nM/16 nM) inhibitor. It has good biological activity and kinase specificity. |
| In vitro | CX-6258 shows antiproliferative activity against a panel of human cancer cell lines with IC50 of 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 with combination index (CI50) values equal to 0.4 and 0.56, respectively. CX-6258 causes dose dependent inhibition of the phosphorylation of two pro-survival proteins, Bad and 4E-BP1, at the Pim kinase specific sites S112 and S65 and T37/46, respectively. [1] |
| Target activity | Pim3:16 nM, Pim1:5 nM, Pim2:25 nM |
| Synonyms | CX 6258 |
| molecular weight | 461.94 |
| Molecular formula | C26H24ClN3O3 |
| CAS | 1202916-90-2 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 22.5 mg/mL (48.71 mM) |
| References | 1. Haddach M, et al. ACS Medicinal Chemistry Letters, 3 (2) , 135-139 |