Identification | Back Directory | [Name]
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 hydrochloride | [CAS]
1160295-21-5 | [Synonyms]
MLN4924 HCl MLN4924 (HCl salt) TAK-924 hydrochloride MLN-4924 hydrochloride Pevonedistat HCl (MLN4924 Pevonedistat hydrochloride PEVONEDISTAT HYDROCHLORIDE;TAK-924 HYDROCHLORIDE PEVONEDISTAT HYDROCHLORIDE;MLN-4924 HYDROCHLORIDE;MLN 4924 HYDROCHLORIDE 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 hydrochloride 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 hydrochloride ISO 9001:2015 REACH | [EINECS(EC#)]
200-258-5 | [Molecular Formula]
C21H26ClN5O4S | [MDL Number]
MFCD17215670 | [MOL File]
1160295-21-5.mol | [Molecular Weight]
479.98 |
Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 100 mg/mL (208.34 mM; Need ultrasonic)H2O : 10 mg/mL (20.83 mM; Need ultrasonic) | [form ]
Powder | [color ]
White to off-white |
Hazard Information | Back Directory | [Uses]
Pevonedistat (MLN4924) hydrochloride is a potent and selective NEDD8-activating enzyme (NAE) inhibitor, with an IC50 of 4.7 nM. Pevonedistat hydrochloride induces the deregulation of S-phase DNA synthesis, thereby disrupting protein turnover mediated by cullin-RING ligase, leading to apoptosis of human tumor cells. Pevonedistat hydrochloride suppresses the growth of human tumour xenografts in mice[1]. | [in vivo]
Pevonedistat (MLN492410, 30 or 60 mg/kg, s.c.) leads to a dose- and time-dependent increase in the steady state levels of NRF2 and CDT1 in HCT-116 tumour-bearing mice, and decreases NEDD8-cullin levels in normal mouse tissue as illustrated in mouse bone marrow cells[1]. | [storage]
Store at -20°C | [References]
[1] Soucy TA, et al. An inhibitor of NEDD8-activating enzyme as a new approach to treat cancer. Nature. 2009 Apr 9;458(7239):732-6. DOI:10.1038/nature07884 [2] J. Claire Godbersen, e tal. The Nedd8-Activating Enzyme Inhibitor MLN4924 Thwarts Microenvironment-Driven NF-κB Activation and Induces Apoptosis in Chronic Lymphocytic Leukemia B Cells. DOI:10.1158/1078-0432.CCR-16-1475 [3] Lan H, et al. Neddylation inhibitor MLN4924 suppresses growth and migration of human gastric cancer cells. Sci Rep. 2016 Apr 11;6:24218. DOI:10.1038/srep24218 |
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Company Name: |
SPIRO PHARMA
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Tel: |
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Website: |
www.spiropharma.com.cn |
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