NVP-LCQ195 是CDK杂环类抑制剂，对CDK1，CDK2，CDK3和CDK5的IC50为1到42 nM之间。

NVP-LCQ195 (AT9311) is a potent inhibitor of CDK1, CDK2, CDK3 and CDK5 (IC50: 1-42 nM).

NVP-LCQ195 induced cell cycle arrest and eventual apoptotic cell death of MM cells, even at sub-1 mol/l concentrations, spared non-malignant cells, and overcame the protection conferred to MM cells by stroma or cytokines of the bone marrow milieu. In MM cells, LCQ195 triggered decreased amplitude of transcriptional signatures associated with oncogenesis, drug resistance and stem cell renewal, including signatures of activation of key transcription factors for MM cells e.g. myc, HIF-1a, IRF4[1].

Bortezomib-treated MM patients whose tumours had high baseline expression of genes suppressed by LCQ195 had significantly shorter progression-free and overall survival than those with low levels of these transcripts in their MM cells[1].

902156-99-4

C17H19Cl2N5O4S

460.34

AT9311;LCQ-195

H2O:Insoluble
H2O:Insoluble
DMSO:100 mg/mL (217.24 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years