生物活性 NVP-LCQ195 (AT9311; LCQ195) is a small molecule heterocyclic inhibitor of CDK1, CDK2, CDK3 and CDK5 with IC50 of 1-42 nM. IC50 Value: 1 nM(CDK5/p25 and CDK5/p35); 2 nM(CDK1/cyclinB and CDK2/cyclinA); 5 nM(CDK2/cyclinE); 42 nM(CDK3/cyclinE) Target: CDKs LCQ195 induced cell cycle arrest and eventual apoptotic cell death of MM cells, even at sub-lmol/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. 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. These observations provide insight into the biological relevance of multi-targeted CDK inhibition in MM.
分子量 460.33
性状 Solid
Formula C17H19Cl2N5O4S
CAS 号 902156-99-4
运输条件 Room temperature in continental US; may vary elsewhere.
储存方式 Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month 溶解性数据 In Vitro: DMSO : 66.67 mg/mL (144.83 mM; Need ultrasonic)
配制储备液 浓度溶剂体积质量 1 mg 5 mg 10 mg 1 mM 2.1724 mL 10.8618 mL 21.7235 mL 5 mM 0.4345 mL 2.1724 mL 4.3447 mL 10 mM 0.2172 mL 1.0862 mL 2.1724 mL * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂: