S87159 |
NVP-LCQ195 |
源叶(MedMol) | 98% |
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- 产品描述: NVP-LCQ195 (AT9311) is a potent inhibitor of CDK1, CDK2, CDK3 and CDK5 (IC50: 1-42 nM).
- 靶点: CDK
- 体外研究:
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.
- 体内研究:
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.
- 参考文献:
1. McMillin DW, Delmore J, Negri J et al. Molecular and cellular effects of multi-targeted cyclin-dependent kinase inhibition in myeloma: biological and clinical implications. Br J Haematol. 2011 Feb;152(4):420-32.
- 溶解性: Soluble in DMSO
- 保存条件: -20℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 2.172 ml 10.862 ml 21.724 ml 5 mM 0.434 ml 2.172 ml 4.345 ml 10 mM 0.217 ml 1.086 ml 2.172 ml 50 mM 0.043 ml 0.217 ml 0.434 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)