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TAS4464

  Cat. No.:  DC60190   Featured
Chemical Structure
1848959-10-3
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More than 5000 active chemicals with high quality for research!
Field of application
TAS4464 is a highly potent and selective inhibitor of NEDD8 (IC50 of 0.955 nM). TAS4464 selectively inhibited NAE relative to the other E1s UAE and SAE. TAS4464 treatment inhibited cullin neddylation and subsequently induced the accumulation of CRL substrates such as CDT1, p27, and phosphorylated IκBα in human cancer cell lines. TAS4464 showed greater inhibitory effects than those of the known NAE inhibitor MLN4924 both in enzyme assay and in cells.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1848959-10-3
Chemical Name: 7H-Pyrrolo[2,3-d]pyrimidin-4-amine, 7-[5-[(aminosulfonyl)amino]-5-deoxy-beta-D-ribofuranosyl]-5-[2-(2-ethoxy-6-fluorophenyl)ethynyl]-
Synonyms: TAS4464;7H-Pyrrolo[2,3-d]pyrimidin-4-amine, 7-[5-[(aminosulfonyl)amino]-5-deoxy-beta-D-ribofuranosyl]-5-[2-(2-ethoxy-6-fluorophenyl)ethynyl]-;BDBM320991;US10174040, Example 55;4-Amino-7-[(2R,3R,4S,5R)-3,4-dihydroxy-5-[(sulfamoylamino)methyl]tetrahydrofuran-2-yl]-5-[2-(2-ethoxy-6-fluoro-phenyl)ethynyl]pyrrolo[2,3-d]pyrimidine
SMILES: CCOC1=C(C#CC2C3=C(N=CN=C3N)N(C=2)[C@H]4[C@H](O)[C@H](O)[C@@H](CNS(=O)(N)=O)O4)C(F)=CC=C1
Formula: C21H23FN6O6S
M.Wt: 506.5073
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: TAS4464 is a highly potent and selective inhibitor of NEDD8 activating enzyme (NAE), with an IC50 of 0.955 nM[1].
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.
References: [1]. Yoshimura C, et al. TAS4464, a highly potent and selective inhibitor of NEDD8 activating enzyme, suppresses neddylation and shows antitumor activity in diverse cancer models. Mol Cancer Ther. 2019 May 15.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
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