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Pevonedistat hydrochloride

产品编号 T16117 CAS 1160295-21-5

别名: MLN4924 hydrochloride

Pevonedistat hydrochloride is an effective and selective inhibitor of NEDD8-activating enzyme (IC50: 4.7 nM).

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Pevonedistat hydrochloride Chemical Structure

Pevonedistat hydrochloride, CAS 1160295-21-5

规格	价格/CNY	货期
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

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Pevonedistat hydrochloride 的其他形式现货产品:

Pevonedistat

其他形式的 Pevonedistat hydrochloride:

Pevonedistat
现货

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生物活性

化学信息

存储 & 溶解度

参考文献

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

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 100 mg/mL (208.34 mM), Sonication is recommended.

H2O: 10 mg/mL (20.83 mM), Sonication is recommended.

溶液配制表

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
DMSO	100 mM	0.0208 mL	0.1042 mL	0.2083 mL	0.5209 mL

计算器

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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. J. Claire Godbersen, e tal. The Nedd8-Activating Enzyme Inhibitor MLN4924 Thwarts Microenvironment-Driven NF-κB Activation and Induces Apoptosis in Chronic Lymphocytic Leukemia B Cells. 3. Lan H, et al. Neddylation inhibitor MLN4924 suppresses growth and migration of human gastric cancer cells. Sci Rep. 2016 Apr 11;6:24218.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

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。

第一步：请输入动物实验的基本信息

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第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

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