CX-6258

Short Summary : Pan-Pim kinases Inhibitor

Category : Chromatin/Epigenetics|Pim

Purity : 0.9852

CAS Number : 1202916-90-2

Formula : C26H24ClN3O3

Molecular Weight : 461.94

SMILE : CN1CCCN(C(C2=CC(C3=CC=C(/C=C4C(C=C(Cl)C=C5)=C5NC4=O)O3)=CC=C2)=O)CC1

Solubility : >11.15mg/mL in DMSO

Storage : Store at -20°C

Description : 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].
Clinical trial: No clinical data are available
Reference:[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.

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