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Pevonedistat hydrochloride

Catalog No. T16117 CAS 1160295-21-5

Synonyms: 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

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2 mg	5 days	$ 65.00

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Biological Description

Chemical Properties

Storage & Solubility Information

Description	Pevonedistat hydrochloride is an effective and selective inhibitor of NEDD8-activating enzyme (IC50: 4.7 nM).
Targets&IC50	NAE:4.7 nM
In vitro	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].
In vivo	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].

Synonyms	MLN4924 hydrochloride
Molecular Weight	479.98
Formula	C21H26ClN5O4S
CAS No.	1160295-21-5

Storage

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

Solubility Information

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

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

References and Literature

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.

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You can also refer to dose conversion for different animals. More

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Pevonedistat hydrochloride 1160295-21-5 Others Pevonedistat Hydrochloride MLN4924 hydrochloride MLN 4924 Hydrochloride MLN-4924 Hydrochloride MLN4924 Hydrochloride inhibitor inhibit

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