[CAS NO. 1848959-11-4] TAS4464hydrochloride

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PRODUCTS SPECIFICATIONS [1848959-11-4]

Catalog

HY-128586A

Brand

MCE

CAS

1848959-11-4

MDL	MFCD32067968
Molecular Weight	542.97
Molecular Formula	C21H24ClFN6O6S
SMILES	NC1=NC=NC2=C1C(C#CC3=C(F)C=CC=C3OCC)=CN2[C@@H]4O[C@H](CNS(=O)(N)=O)[C@@H](O)[C@H]4O.Cl

For research use only. We do not sell to patients.

TAS4464 (hydrochloride) is a highly potent and selective inhibitor of NEDD8 activating enzyme (NAE) , with an IC ₅₀ of 0.955 nM ^[1] .

IC50：0.955 nM (NAE) ^[1]

NCT Number	Sponsor	Condition	Start Date	Phase
NCT02978235	Taiho Oncology, Inc.	Multiple Myeloma\|NonHodgkin Lymphoma	March 1, 2017	Phase 1

Solid

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

In Vitro:

DMSO : 83.33 mg/mL ( 153.47 mM ; Need ultrasonic)

H ₂ O : 5 mg/mL ( 9.21 mM ; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.08 mg/mL (3.83 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.08 mg/mL (3.83 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.08 mg/mL (3.83 mM); Clear solution

* All of the co-solvents are available by MCE.