CX-6258 hydrochloride 是一种强效选择性的泛 Pim 激酶抑制剂，对Pim-1、Pim-2 和 Pim-3 作用的IC50值分别为 5、25 和 16 nM。

CX-6258 HCl is an effective, orally efficacious Pim1/2/3 kinase inhibitor (IC50: 5/25/16 nM).

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 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.

Pim-1 and Pim-2 inhibitions are measured in radiometric assays using human recombinant Pim-1 at [ATP] = 30 μM (substrate RSRHSSYPAGT) and human recombinant Pim-2 at [ATP] = 5 μM (substrate RSRHSSYPAGT). The radiometric assay for Pim-3 uses RSRHSSYPAGT as a substrate in the presence of [ATP] = 155 μM.

1353859-00-3

C26H25Cl2N3O3

498.4

Pim-Kinase Inhibitor X;CX-6258 HCl

DMSO:53 mg/mL (106.3 mM)
Ethanol:1 mg/mL (2.0 mM),warmed
H2O:82 mg/mL (164.5 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years