产品说明书
LCL161
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同义名 : | NVP-LCL161 |
| CAS号 : | 1005342-46-0 | |
| 货号 : | A188719 | |
| 分子式 : | C26H33FN4O3S | |
| 纯度 : | 99%+ | |
| 分子量 : | 500.629 | |
| MDL号 : | MFCD23160049 | |
| 存储条件： |
粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 105 mg/mL(209.74 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 靶点 |
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| 描述 | LCL161 is an IAP family inhibitor which can bind and inhibit both XIAP and cIAP. Treatment with LCL161 could enhance the activity of different proapoptotic signaling pathways[1]. LCL-161 at concentration of 2μM could induce cIAP degradation and activated downstream NFκB in Eμ-Myc cells[2]. Treatment with LCL161 at concentration<10μM for 24h did not significantly affect protein level of XIAP protein level as Smac-mimetic treatment did not degrade XIAP, but can still inhibit the activity of XIAP measured by upregulation of cleaved caspases 9 and 3, in H929, MM1R and MM1S cells. LCL161 at concentration<15μM dose-dependently induced cell death of H929 and MM1S cells primarily driven by activation of the extrinsic apoptotic pathway[3]. Combination of LCL161 (100mg/kg) with nilotinib showed synergistic effects and significantly delayed the onset of disease recurrence in a BCR-ABL-positive leukemia model[1]. | ||
| 作用机制 | LCL-161 is a SMAC mimetic which can both disengage IAPs from caspases and induce proteasomal degradation of cIAP-1 and -2.[2] | ||
| 细胞研究 | |||||
|---|---|---|---|---|---|
| 细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
| human AGS cells | 2.5 μM | Apoptosis assay | 5 days | Induction of sensitization of human AGS cells to conatumumab-induced apoptosis assessed as cell viability at 2.5 uM after 5 days by MTS assay | 24093940 |
| human BxPC3 cells | 3.3 μM | Cytotoxic assay | 5 days | Potentiation of conatumumab-induced cytotoxicity against human BxPC3 cells at 3.3 uM after 5 days by MTS assay | 24083782 |
| human Capan1 cells | 2.5 μM | Cytotoxic assay | 5 days | Potentiation of conatumumab-induced apoptosis in human Capan1 cells at 2.5 uM after 5 days by MTS assay | 24093940 |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.00mL 0.40mL 0.20mL |
9.99mL 2.00mL 1.00mL |
19.97mL 3.99mL 2.00mL |
