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TAS4464 E1 Activating inhibitor

Name: TAS4464
Brand: Selleck Chemicals
SKU: S8849
Availability: InStock
Rating: 5 (2 reviews)

Cat.No.S8849

TAS4464 is a potent and highly selective NEDD8 activating enzyme (NAE) inhibitor with IC50 of 0.955 nM. This compound exhibits superior antitumor activity with prolonged target inhibition.

Chemical Structure

Molecular Weight: 506.51

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Quality Control

Batch: Purity: 99.07%

99.07

Related Targets	Proteasome E3 Ligase DUB p97 SUMO E2 conjugating
Other E1 Activating Products	MLN4924 (Pevonedistat) TAK-243 (MLN7243) PYR-41 ML792 COH000 Pevonedistat hydrochloride Ubiquitin Antibody [J9C13] PYZD-4409 Atg7 Antibody [K21F3] NEDD8 Antibody [D22F6]

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (197.42 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (9.87mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.500mg/ml (0.99mM)	Taking the 1 mL working solution as an example, add 50 μL of 10 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

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 addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	506.51	Formula	C₂₁H₂₃FN₆O₆S	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	1848959-10-3	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CCOC1=CC=CC(=C1C#CC2=C[N](C3OC(CN[S](N)(=O)=O)C(O)C3O)C4=C2C(=NC=N4)N)F

Mechanism of Action

Targets/IC₅₀/Ki	NAE (Cell-free assay) 0.955 nM
In vitro	TAS4464 selectively inhibits NAE relative to the other E1s UAE and SAE. This compound treatment inhibits cullin neddylation and subsequently induces the accumulation of CRL substrates such as CDT1, p27, and phosphorylated IkBa in human cancer cell lines. Cytotoxicity profiling reveals that it is highly potent with widespread antiproliferative activity not only for cancer cell lines, but also patient-derived tumor cells.
In vivo	TAS4464 shows prolonged target inhibition in human tumor xenograft mouse models; weekly or twice a week administration of this compound led to prominent antitumor activity in multiple human tumor xenograft mouse models including both hematologic and solid tumors without marked weight loss.
References	[1] https://pubmed.ncbi.nlm.nih.gov/31092565/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT02978235	Terminated	Multiple Myeloma\|NonHodgkin Lymphoma	Taiho Oncology Inc.	March 1 2017	Phase 1

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