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Pevonedistat

Chemical Structure : Pevonedistat

CAS No.: 905579-51-3

Pevonedistat (MLN4924, TAK-924 )

Catalog No.: PC-45949Not For Human Use, Lab Use Only.

MLN4924 (Pevonedistat, TAK-924) is an analog of adenosine 5’-monophosphate that potently and selectively inhibits NEDD8-activating enzyme (NAE) with IC50 of 4.7 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

MLN4924 (Pevonedistat, TAK-924) is an analog of adenosine 5’-monophosphate that potently and selectively inhibits NEDD8-activating enzyme (NAE) with IC50 of 4.7 nM.
MLN4924 (Pevonedistat, TAK-924) also inhibits the related enzymes ubiquitin-activating enzyme (UAE) and SUMO-activating enzyme (SAE) with IC50 of 1.5 and 8.2 uM, respectively.
MLN4924 (Pevonedistat, TAK-924) disrupts CRL-mediated protein turnover leading to apoptosis in HCT116 cells, suppresses the growth of human tumor xenografts in mice (30-60 mg/kg).

Physicochemical Properties

M.Wt 443.5193
Formula C21H25N5O4S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
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Solubility

DMSO: ≥ 111.25 mg/mL

Chemical Name/SMILES

Sulfamic acid, [(1S,2S,4R)-4-[4-[[(1S)-2,3-dihydro-1H-inden-1-yl]amino]-7H-pyrrolo[2,3-d]pyrimidin-7-yl]-2-hydroxycyclopentyl]methyl ester

References

1. Soucy TA, et al. Nature. 2009 Apr 9;458(7239):732-6.

2. Milhollen MA, et al. Blood. 2010 Sep 2;116(9):1515-23.

3. Brownell JE, et al. Mol Cell. 2010 Jan 15;37(1):102-11.

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