产品描述: | Pevonedistat (MLN4924) is a potent and selective NEDD8-activating enzyme (NAE) inhibitor with an IC50 of 4.7 nM |
靶点: |
IC50: 4.7 nM (NAE);E1/E2/E3Enzyme; NEDD8 |
体内研究: |
Pevonedistat (MLN4924) (sc, 10 mg/kg, 30 mg/kg, or 60 mg/kg) inhibits the NEDD8 pathway resulting in DNA damage in Mice bearing HCT-116 xenografts.Pevonedistat (sc, 120 mg/kg) and TNF-α (10 μg/kg) synergistically cause liver damage in SD rats |
参考文献: |
1. Soucy TA, et al. An inhibitor of NEDD8-activating enzyme as a new approach to treat cancer. Nature. 2009 Apr 9;458(7239):732-6. 2. F S Wolenski, et al. The NAE inhibitor pevonedistat (MLN4924) synergizes with TNF-α to activate apoptosis. Cell Death Discovery 1, Article number: 15034 (2015) |
溶解性: |
DMSO : 62.5 mg/mL (140.92 mM; Need ultrasonic) |
保存条件: |
-20℃ |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
2.255 ml |
11.273 ml |
22.546 ml |
5 mM |
0.451 ml |
2.255 ml |
4.509 ml |
10 mM |
0.225 ml |
1.127 ml |
2.255 ml |
50 mM |
0.045 ml |
0.225 ml |
0.451 ml |
|
注意: |
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