Pevonedistat HCl (MLN-4924; TAK-924)

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

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Size	Price	Stock
250mg	$1450	Check With Us
500mg	$2080	Check With Us
1g	$3120	Check With Us

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Cat #: V3202 CAS #: 1160295-21-5 Purity ≥ 98%

Description: Pevonedistat HCl (MLN4924; TAK924), the hydrochloride salt of Pevonedistat, is an inhibitor of Nedd8 (Neural precursor cell expressed, developmentally down-regulated 8) activating enzyme (NAE) with IC50 of 4 nM.

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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Physicochemical and Storage Information
Protocol
Related Biological Data
Stock Solution Preparation
Quality Control Documentation

Molecular Weight (MW)	479.98
Molecular Formula	C21H26ClN5O4S
CAS No.	1160295-21-5
Storage	-20℃ for 3 years in powder formr
Storage	-80℃ for 2 years in solvent
Solubility In Vitro	DMSO: >100 mg/mLr
	Water: N/Ar
	Ethanol: N/A
SMILES Code	[H]Cl.O=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
Synonyms	MLN-4924 HCl; TAK 924 HCl; MLN4924 HCl; TAK924 HCl; Pevonedistat HCl; TAK-924 HCl

Protocol	In Vitro	Pevonedistat (MLN4924) is a potent 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) treatment inhibits overall protein turnover in cultured HCT-116 cells. Treatment of HCT-116 cells with Pevonedistat (MLN4924) for 24 h results in a dose-dependent decrease of Ubc12-NEDD8 thioester and NEDD8-cullin conjugates, with an 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.
Protocol	In Vivo	Pevonedistat (MLN492410, 30 or 60 mg/kg, s.c.) leads to a dose- and time-dependent increase in the steady state levels of NRF2 and CDT1 in HCT-116 tumour-bearing mice, and decreases NEDD8-cullin levels in normal mouse tissue as illustrated in mouse bone marrow cells. Pevonedistat (MLN4924) administered on a BID schedule at 30 and 60 mg/kg inhibits tumour growth with T/C values of 0.36 and 0.15, respectively.

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	1mg	5mg	10mg	20mg
1mM	2.0834 mL	10.4171 mL	20.8342 mL	41.6684 mL
5mM	0.4167 mL	2.0834 mL	4.1668 mL	8.3337 mL
10mM	0.2083 mL	1.0417 mL	2.0834 mL	4.1668 mL
20mM	0.1042 mL	0.5209 mL	1.0417 mL	2.0834 mL

Quality Control Documentation	Select Batch Purity ≥ 98% COA MSDS NMR HPLC

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)

Volume_(start)

Concentration_(final)

Volume_(final)

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.