Reagenti e strumenti per immunologia, biologia cellulare e biologia molecolare

Pevonedistat [905579-51-3]

Stampa

Cat# HY-70062-1ml

Size : 10mM/1mL

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Telefono : +1 850 650 7790

Marca : MedChemExpress

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Contatta il distributore locale :

Telefono : +1 850 650 7790

Description

Pevonedistat (MLN4924) is a potent and selective NEDD8-activating enzyme (NAE) inhibitor with an IC₅₀ of 4.7 nM^[1].

IC₅₀ & Target

IC50: 4.7 nM (NAE)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	0.63 μM Compound: MLN4924	Antiproliferative activity against human A549 cells incubated for 48 hrs by CCK-8 assay Antiproliferative activity against human A549 cells incubated for 48 hrs by CCK-8 assay	[PMID: 33129593]
A549	IC₅₀	47.79 μM Compound: MLN4924	Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 34624825]
BEAS-2B	IC₅₀	1.22 μM Compound: MLN4924	Cytotoxicity against human BEAS-2B cells incubated for 48 hrs by CCK-8 assay Cytotoxicity against human BEAS-2B cells incubated for 48 hrs by CCK-8 assay	[PMID: 33129593]
Caco-2	IC₅₀	4.4 μM Compound: MLN4924	Cytotoxicity against human Caco2 cells after 72 hrs by MTT assay Cytotoxicity against human Caco2 cells after 72 hrs by MTT assay	[PMID: 29232579]
CAPAN-1	IC₅₀	101 nM Compound: 1; MLN4924	Antiproliferative activity against human CAPAN-1 cells assessed as cell growth inhibition measured after 72 hrs by SRB assay Antiproliferative activity against human CAPAN-1 cells assessed as cell growth inhibition measured after 72 hrs by SRB assay	[PMID: 33857374]
DU-145	IC₅₀	201 nM Compound: 1; MLN4924	Antiproliferative activity against human DU-145 cells assessed as cell growth inhibition measured after 72 hrs by SRB assay Antiproliferative activity against human DU-145 cells assessed as cell growth inhibition measured after 72 hrs by SRB assay	[PMID: 33857374]
EKVX	IC₅₀	> 10 μM Compound: MLN4924	Antiproliferative activity against human EKVX cells measured after 48 hrs by CCK8 assay Antiproliferative activity against human EKVX cells measured after 48 hrs by CCK8 assay	[PMID: 31732254]
EKVX	IC₅₀	0.3 μM Compound: MLN4924	Antiproliferative activity against human EKVX cells measured after 72 to 96 hrs by CCK8 assay Antiproliferative activity against human EKVX cells measured after 72 to 96 hrs by CCK8 assay	[PMID: 31732254]
GES1	IC₅₀	13.45 μM Compound: MLN4924	Cytotoxicity against human GES1 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Cytotoxicity against human GES1 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 34624825]
HCT-116	IC₅₀	0.19 μM Compound: MLN4924	Antitumor activity against human HCT116 cells after 72 hrs by MTT assay Antitumor activity against human HCT116 cells after 72 hrs by MTT assay	[PMID: 28388520]
HCT-116	IC₅₀	33.89 nM Compound: 1; MLN4924	Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition by sulforhodamine B assay Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition by sulforhodamine B assay	[PMID: 33857374]
HCT-116	IC₅₀	36.2 nM Compound: 1; MLN4924	Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition measured after 72 hrs by SRB assay Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition measured after 72 hrs by SRB assay	[PMID: 33857374]
HepG2	IC₅₀	> 10 μM Compound: MLN4924	Antiproliferative activity against human HepG2 cells measured after 48 hrs by CCK8 assay Antiproliferative activity against human HepG2 cells measured after 48 hrs by CCK8 assay	[PMID: 31732254]
HepG2	IC₅₀	0.3 μM Compound: MLN4924	Antiproliferative activity against human HepG2 cells measured after 72 to 96 hrs by CCK8 assay Antiproliferative activity against human HepG2 cells measured after 72 to 96 hrs by CCK8 assay	[PMID: 31732254]
HepG2	IC₅₀	8.15 μM Compound: MLN4924	Antiproliferative activity against human HepG2 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 34624825]
HGC-27	IC₅₀	1.25 μM Compound: MLN4924	Antiproliferative activity against human HGC-27 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against human HGC-27 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 34624825]
HT-29	IC₅₀	484 nM Compound: 1; MLN4924	Antiproliferative activity against human HT-29 cells assessed as cell growth inhibition measured after 72 hrs by SRB assay Antiproliferative activity against human HT-29 cells assessed as cell growth inhibition measured after 72 hrs by SRB assay	[PMID: 33857374]
Huh-7	IC₅₀	> 10 μM Compound: MLN4924	Antiproliferative activity against human HuH7 cells measured after 48 hrs by CCK8 assay Antiproliferative activity against human HuH7 cells measured after 48 hrs by CCK8 assay	[PMID: 31732254]
Huh-7	IC₅₀	0.3 μM Compound: MLN4924	Antiproliferative activity against human HuH7 cells measured after 72 to 96 hrs by CCK8 assay Antiproliferative activity against human HuH7 cells measured after 72 to 96 hrs by CCK8 assay	[PMID: 31732254]
HuTu80	IC₅₀	42.6 nM Compound: 1; MLN4924	Antiproliferative activity against human HuTu80 cells assessed as cell growth inhibition measured after 72 hrs by SRB assay Antiproliferative activity against human HuTu80 cells assessed as cell growth inhibition measured after 72 hrs by SRB assay	[PMID: 33857374]
Jurkat	IC₅₀	152 nM Compound: 1; MLN4924	Antiproliferative activity against human Jurkat cells assessed as cell growth inhibition measured after 72 hrs by SRB assay Antiproliferative activity against human Jurkat cells assessed as cell growth inhibition measured after 72 hrs by SRB assay	[PMID: 33857374]
K562	EC₅₀	108 nM Compound: 2, MLN4924	Antiproliferative activity against human K562 cells after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human K562 cells after 72 hrs by CellTiter-Glo assay	[PMID: 24900352]
LNCaP-Clone-FGC	IC₅₀	64.6 nM Compound: 1; MLN4924	Antiproliferative activity against human LNCaP-Clone-FGC cells assessed as cell growth inhibition measured after 72 hrs by SRB assay Antiproliferative activity against human LNCaP-Clone-FGC cells assessed as cell growth inhibition measured after 72 hrs by SRB assay	[PMID: 33857374]
MCF7	IC₅₀	> 10 μM Compound: MLN4924	Antiproliferative activity against human MCF7 cells measured after 48 hrs by CCK8 assay Antiproliferative activity against human MCF7 cells measured after 48 hrs by CCK8 assay	[PMID: 31732254]
MCF7	IC₅₀	> 100 μM Compound: MLN4924	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 34624825]
MCF7	IC₅₀	0.3 μM Compound: MLN4924	Antiproliferative activity against human MCF7 cells measured after 72 to 96 hrs by CCK8 assay Antiproliferative activity against human MCF7 cells measured after 72 to 96 hrs by CCK8 assay	[PMID: 31732254]
MGC-803	IC₅₀	> 10 μM Compound: MLN4924	Antiproliferative activity against human MGC803 cells measured after 48 hrs by CCK8 assay Antiproliferative activity against human MGC803 cells measured after 48 hrs by CCK8 assay	[PMID: 31732254]
MGC-803	IC₅₀	0.3 μM Compound: MLN4924	Antiproliferative activity against human MGC803 cells measured after 72 to 96 hrs by CCK8 assay Antiproliferative activity against human MGC803 cells measured after 72 to 96 hrs by CCK8 assay	[PMID: 31732254]
MGC-803	IC₅₀	5.16 μM Compound: MLN4924	Antiproliferative activity against human MGC-803 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against human MGC-803 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 34624825]
MKN-45	IC₅₀	> 10 μM Compound: MLN4924	Antiproliferative activity against human MKN45 cells measured after 48 hrs by CCK8 assay Antiproliferative activity against human MKN45 cells measured after 48 hrs by CCK8 assay	[PMID: 31732254]
MKN-45	IC₅₀	0.3 μM Compound: MLN4924	Antiproliferative activity against human MKN45 cells measured after 72 to 96 hrs by CCK8 assay Antiproliferative activity against human MKN45 cells measured after 72 to 96 hrs by CCK8 assay	[PMID: 31732254]
MV4-11	IC₅₀	107 nM Compound: 1; MLN4924	Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition measured after 72 hrs by SRB assay Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition measured after 72 hrs by SRB assay	[PMID: 33857374]
NCI-H1299	IC₅₀	> 10 μM Compound: MLN4924	Antiproliferative activity against human H1299 cells measured after 48 hrs by CCK8 assay Antiproliferative activity against human H1299 cells measured after 48 hrs by CCK8 assay	[PMID: 31732254]
NCI-H1299	IC₅₀	0.3 μM Compound: MLN4924	Antiproliferative activity against human H1299 cells measured after 72 to 96 hrs by CCK8 assay Antiproliferative activity against human H1299 cells measured after 72 to 96 hrs by CCK8 assay	[PMID: 31732254]
NCI-H1299	IC₅₀	0.49 μM Compound: MLN4924	Antiproliferative activity against human H1299 cells incubated for 48 hrs by CCK-8 assay Antiproliferative activity against human H1299 cells incubated for 48 hrs by CCK-8 assay	[PMID: 33129593]
PLC	IC₅₀	> 10 μM Compound: MLN4924	Antiproliferative activity against human PLC cells measured after 48 hrs by CCK8 assay Antiproliferative activity against human PLC cells measured after 48 hrs by CCK8 assay	[PMID: 31732254]
PLC	IC₅₀	0.3 μM Compound: MLN4924	Antiproliferative activity against human PLC cells measured after 72 to 96 hrs by CCK8 assay Antiproliferative activity against human PLC cells measured after 72 to 96 hrs by CCK8 assay	[PMID: 31732254]
RKO	IC₅₀	166 nM Compound: 1; MLN4924	Antiproliferative activity against human RKO cells assessed as cell growth inhibition measured after 72 hrs by SRB assay Antiproliferative activity against human RKO cells assessed as cell growth inhibition measured after 72 hrs by SRB assay	[PMID: 33857374]
T47D	IC₅₀	> 10 μM Compound: MLN4924	Antiproliferative activity against human T47D cells measured after 48 hrs by CCK8 assay Antiproliferative activity against human T47D cells measured after 48 hrs by CCK8 assay	[PMID: 31732254]
T47D	IC₅₀	0.3 μM Compound: MLN4924	Antiproliferative activity against human T47D cells measured after 72 to 96 hrs by CCK8 assay Antiproliferative activity against human T47D cells measured after 72 to 96 hrs by CCK8 assay	[PMID: 31732254]
THP-1	IC₅₀	115 nM Compound: 1; MLN4924	Antiproliferative activity against human THP-1 cells assessed as cell growth inhibition measured after 72 hrs by SRB assay Antiproliferative activity against human THP-1 cells assessed as cell growth inhibition measured after 72 hrs by SRB assay	[PMID: 33857374]
U2OS	IC₅₀	0.16 μM Compound: MLN4924	Antitumor activity against human U2OS cells after 72 hrs by MTT assay Antitumor activity against human U2OS cells after 72 hrs by MTT assay	[PMID: 28388520]

In Vitro

Pevonedistat (MLN4924) is a potent inhibitor of NAE, 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) when evaluated in purified enzyme assays that monitor the formation of E2-UBL thioester reaction products. Pevonedistat (MLN4924) selectively inhibits NAE activity compared to the closely related ubiquitin-activating enzyme (UAE, also known as UBA1) and SUMO-activating enzyme (SAE; a heterodimer of SAE1 and UBA2 subunits), in purified enzyme and cellular assays. MLN4924 exhibits potent cytotoxic activity against a variety of human tumour-derived cell lines^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Solvant et solubilité

In Vitro:

DMSO : 62.5 mg/mL (140.92 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.2547 mL	11.2734 mL	22.5469 mL
5 mM	0.4509 mL	2.2547 mL	4.5094 mL
10 mM	0.2255 mL	1.1273 mL	2.2547 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Saline
Solubility: 5 mg/mL (11.27 mM); Suspended solution; Need ultrasonic
Protocol 2

Add each solvent one by one: 5% DMSO 95% Saline
Solubility: 2.5 mg/mL (5.64 mM); Suspended solution; Need ultrasonic
Protocol 3

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.69 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 4

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.69 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 5

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (4.69 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.
Protocol 6

Add each solvent one by one: 1% DMSO 99% Saline
Solubility: 0.5 mg/mL (1.13 mM); Suspended solution; Need ultrasonic

Pureté et documentation

Purity: 99.98%

Fiche technique (283 KB) SDS (393 KB)

COA (254 KB) HNMR (547 KB) RP-HPLC (214 KB) LCMS (109 KB)

Instruction de manipulation (2659 KB)

Références

[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. [Content Brief]

[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)

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