Molecular Formula | C26H25Cl2N3O3 |
Molar Mass | 498.4 |
Storage Condition | Inert atmosphere,Room Temperature |
In vitro study | CX-6258 showed anti-proliferative activity against a panel of human cancer cell lines with an IC50 of 0.02-3.7 μm, most sensitive to acute leukemia cell lines. CX-6258 combined with doxorubicin (10:1 molar ratio), and CX-6258 combined with paclitaxel (100:1 molar ratio) produced synergistic cell killing, Composite Index (CI50). Values were 0.4 and 0.56, respectively. CX-6258 dose-dependently inhibited the phosphorylation of two pro-survivin proteins, Bad and 4E-BP1, at specific sites of Pim kinase S112 and S65 and T37/46, respectively. CX-6258 showed antiproliferative activity against a panel of human cancer cell lines with an IC50 of 0.02-3.7 μm, most sensitive to acute leukemia cell lines. CX-6258 combined with doxorubicin (10:1 molar ratio), and CX-6258 combined with paclitaxel (100:1 molar ratio) produced synergistic cell killing, Composite Index (CI50). Values were 0.4 and 0.56, respectively. CX-6258 dose-dependently inhibited the phosphorylation of two pro-survivin proteins, Bad and 4E-BP1, at specific sites of Pim kinase S112 and S65 and T37/46, respectively. |
In vivo study | CX-6258 showed dose-dependent efficacy, inhibiting tumor growth in MV-4-11 of xenografted mice, and producing 45% tumor growth inhibition (TGI) at a dose of 50 mg/kg, the 100 mg/kg dose produced 75% TGI CX-6258 showing dose-dependent efficacy in inhibiting tumor growth in xenografted mice by MV-4-11, the 50 mg/kg dose produced 45% tumor growth inhibition (TGI) and the 100 mg/kg dose produced 75% TGI |