atiprimod dimaleate

Atiprimod Dimaleate is a JAK2 inhibitor.

Atiprimod is an orally bioavailable small molecule belonging to the azaspirane class of cationic amphiphilic agents with anti-inflammatory, antineoplastic, and antiangiogenic properties. Atiprimod inhibits the phosphorylation of signal transducer and activator of transcription 3 (STAT3), blocking the signalling pathways of interleukin-6 and vascular endothelial growth factor (VEGF) and downregulating the anti-apoptotic proteins Bcl-2, Bcl-XL, and Mcl-1, thereby inhibiting cell proliferation, inducing cell cycle arrest, and inducing apoptosis.

JAK2 inhibitor (IC50 = 397 nM). Also inhibits STAT3 and STAT5 phosphorylation. Inhibits cell growth and induces apoptosis in cells expressing the JAK2V617F mutation. Manshouri et al (2011) Bone marrow stroma-secreted cytokines protect JAK2(V617F)-mutated cells from the effects of a JAK2 inhibitor. Cancer Res. 71 3831 PMID:21512135 |Quintás-Cardama et al (2011) Preclinical characterization of atiprimod, a novel JAK2 AND JAK3 inhibitor. Invest.New Drugs 29 818 PMID:20372971