Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Pevonedistat hydrochloride is an effective and selective inhibitor of NEDD8-activating enzyme (IC50: 4.7 nM).
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 569 | 5日内发货 | ||
5 mg | ¥ 955 | 8-10周 | ||
10 mg | ¥ 1,810 | 8-10周 | ||
100 mg | ¥ 8,290 | 8-10周 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,100 | 8-10周 |
Pevonedistat hydrochloride 的其他形式现货产品:
产品描述 | Pevonedistat hydrochloride is an effective and selective inhibitor of NEDD8-activating enzyme (IC50: 4.7 nM). |
靶点活性 | NAE:4.7 nM |
体外活性 | Pevonedistat is an effective inhibitor of NAE (half-maximal inhibitory concentration (IC50=0.004 μM), and is selective relative to the closely related enzymes UAE, SAE, UBA6 and ATG7 (IC50=1.5, 8.2, 1.8 and >10 μM, respectively). Pevonedistat (MLN4924) rapidly inhibits cullin 1 neddylation and remarkably suppressed growth and survival as well as migration in a dose-and time-dependent manner in gastric cancer cells, and significantly suppresses migration by transcriptionally activating E-cadherin and repressing MMP-9. Pevonedistat induces CLL cell apoptosis and circumvented stroma-mediated resistance. Pevonedistat promotes induction of Bim and Noxa in the CLL cells leading to rebalancing of Bcl-2 family members toward the proapoptotic BH3-only proteins. Pevonedistat treatment inhibits overall protein turnover in cultured HCT-116 cells. Treatment of HCT-116 cells with Pevonedistat for 24 h causes a dose-dependent decrease of Ubc12-NEDD8 thioester and NEDD8-cullin conjugates (IC50 < 0.1 μM) resulting in a reciprocal increase in the abundance of the known CRL substrates CDT1, p27 and NRF2 (also known as NFE2L2), but not non-CRL substrates[1][2][3]. |
体内活性 | Pevonedistat administered on a BID schedule at 30 and 60 mg/kg inhibits tumor growth (T/C: 0.36 and 0.15, respectively). Pevonedistat (30 or 60 mg/kg, s.c.) causes a dose- and time-dependent enhance the steady-state levels of NRF2 and CDT1 in HCT-116 tumor-bearing mice and reduces NEDD8-cullin levels in normal mouse tissue as illustrated in mouse bone marrow cells [1]. |
别名 | MLN4924 hydrochloride |
分子量 | 479.98 |
分子式 | C21H26ClN5O4S |
CAS No. | 1160295-21-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 100 mg/mL (208.34 mM), Sonication is recommended.
H2O: 10 mg/mL (20.83 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / H2O | 1 mM | 2.0834 mL | 10.4171 mL | 20.8342 mL | 52.0855 mL |
5 mM | 0.4167 mL | 2.0834 mL | 4.1668 mL | 10.4171 mL | |
10 mM | 0.2083 mL | 1.0417 mL | 2.0834 mL | 5.2086 mL | |
20 mM | 0.1042 mL | 0.5209 mL | 1.0417 mL | 2.6043 mL | |
DMSO | 50 mM | 0.0417 mL | 0.2083 mL | 0.4167 mL | 1.0417 mL |
100 mM | 0.0208 mL | 0.1042 mL | 0.2083 mL | 0.5209 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Pevonedistat hydrochloride 1160295-21-5 Others Pevonedistat Hydrochloride MLN4924 hydrochloride MLN 4924 Hydrochloride MLN-4924 Hydrochloride MLN4924 Hydrochloride Inhibitor inhibitor inhibit