CX6258

The Uses of CX6258

CX-6258 is a potent, selective, and orally efficacious pan-Pim kinases inhibitor.

Biological Activity

pim kinases (provirus integration site for moloney murine leukemia virus) are a family of serine/threonine kinases that regulate cell survival. this family of kinases is composed of three different isoforms (pim-1, pim-2, and pim-3). the simultaneous inhibition of pim-1, pim-2, and pim-3 kinases is emerging as a promising strategy for anticancer drug development. cx-6258 is a potent, selective, and orally efficacious pan-pim kinases inhibitor.

in vitro

cx-6258 exhibited in vitro synergy with chemotherapeutics. the antiproliferative activity of cx-6258 was examined against a panel of cell lines derived from human solid tumors and hematological malignancies. cx-6258 demonstrated robust antiproliferative potencies against all cell lines tested [1].

in vivo

cx-6258 was evaluated in two human tumor xenograft growth efficacy models, acute myeloid leukemia mv-4-11, and prostate adenocarcinoma pc3. the drug exhibited dose dependent efficacy, with a 50 mg/kg dose producing 45% tumor growth inhibition (tgi) and a 100 mg/kg dose producing 75% tgi. in addition, cx-6258 displayed significant efficacy in vivo in two xenograft models representing the diseases where pim kinases had been shown to play an important role [1].

References

[1] haddach m, michaux j, schwaebe mk, et al. discovery of cx-6258. a potent, selective, and orally efficacious pan-pim kinases inhibitor. acs med chem lett. 2011;3(2):135-9.