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Description: NVP-LCQ195 (formerly also known as AT9311; AT-9311; LCQ195; LCQ-195) is a novel and potent small molecule heterocyclic inhibitor of cyclin-dependent kinases CDK1, CDK2, CDK3 and CDK5 with IC50 of 1-42 nM. LCQ195 induced cell cycle arrest and eventual apoptotic cell death of MM cells, even at sub-umol/l concentrations, spared non-malignant cells, and overcame the protection conferred to MM cells by stroma or cytokines of the bone marrow milieu. Cell cycle regulators, such as cyclin-dependent kinases (CDKs), are appealing targets for multiple myeloma (MM) therapy given the increased proliferative rates of tumour cells in advanced versus early stages of MM.
References: Br J Haematol. 2011 Feb; 152(4):420-32.
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