[CAS NO. 1848959-10-3] TAS4464
PRODUCTS SPECIFICATIONS [1848959-10-3]
DESCRIPTION [1848959-10-3]
Overview
| MDL | MFCD32067967 |
|---|---|
| Molecular Weight | 506.51 |
| Molecular Formula | C21H23FN6O6S |
| 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 |
2 Publications Citing Use of MCE
Summary
TAS4464 is a highly potent and selective inhibitor of NEDD8 activating enzyme (NAE) , with an IC 50 of 0.955 nM [1] .
IC50 & Target
IC50：0.955 nM (NAE) [1]
In Vitro
TAS4464 treatment inhibits cullin neddylation and subsequently induces the accumulation of CRL substrates such as CDT1, p27, and phosphorylates IκBα in 47 human cancer cell lines.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT02978235 | Taiho Oncology, Inc. |
Multiple Myeloma|NonHodgkin Lymphoma
|
March 1, 2017 | Phase 1 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 40 mg/mL ( 78.97 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.9743 mL | 9.8715 mL | 19.7429 mL |
| 5 mM | 0.3949 mL | 1.9743 mL | 3.9486 mL |
| 10 mM | 0.1974 mL | 0.9871 mL | 1.9743 mL |
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Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2 mg/mL (3.95 mM); Clear solution