Pevonedistat (TAK924; MLN4924)

This product is for research use only, not for human use. We do not sell to patients.

Pevonedistat (TAK924; MLN4924)
For small sizes, please check our retail website as below: www.invivochem.com
Size Price Stock
250mg$1450Check With Us
500mg$2080Check With Us
1g$3120Check With Us

Cat #: V2786 CAS #: 905579-51-3 Purity ≥ 98%

Description: Pevonedistat (previously known as MLN-4924; TAK-924) is a potent and selective small molecule inhibitor of Nedd8 (Neural precursor cell expressed, developmentally down-regulated 8) activating enzyme (NAE) with anticancer activity.

References: 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.

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Molecular Weight (MW)443.52
Molecular FormulaC21H25N5O4S
CAS No.905579-51-3
Storage-20℃ for 3 years in powder formr
-80℃ for 2 years in solvent
Solubility In VitroDMSO:88 mg/mL (198.41 mM)r
Water: <1 mg/mLr
Ethanol:88 mg/mL (198.41 mM)
SMILES CodeO=S(OC[C@H]1[C@@H](O)C[C@H](N2C=CC3=C(N[C@H]4CCC5=C4C=CC=C5)N=CN=C32)C1)(N)=O
SynonymsMLN-4924; TAK924; MLN4924; TAK 924; MLN 4924; Pevonedistat; TAK-924
ProtocolIn VitroPevonedistat (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.
In VivoPevonedistat (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.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM2.2547 mL11.2734 mL22.5469 mL45.0938 mL
5mM0.4509 mL2.2547 mL4.5094 mL9.0188 mL
10mM0.2255 mL1.1273 mL2.2547 mL4.5094 mL
20mM0.1127 mL0.5637 mL1.1273 mL2.2547 mL
Quality Control Documentation
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
=
Concentration
×
Volume
×
Molecular Weight*
The dilution calculator equation
Concentration(start) × Volume(start) = Concentration(final) × Volume(final)

This equation is commonly abbreviated as: C1 V1 = C2 V2

Concentration(start)
C1
×
Volume(start)
V1
=
Concentration(final)
C2
×
Volume(final)
V2
Step One: Enter information below
Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals
Step Two: Enter the in vivo formulation
%DMSO + % + %Tween 80 + %ddH2O

Calculation Results:
Working concentration: mg/ml;
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.
Note:
  • (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
  • (2) Be sure to add the solvent(s) in order.