Pevonedistat
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- CAS-Nr.
- 905579-51-3
- Englisch Name:
- Pevonedistat
- Synonyma:
- MLN 4924;CS-821;TAK-924;Pevonedistat;mln4924 Free Base;PEVONEDISTAT;MLN-4924;MLN4924 (Pevonedistat);Pevonedistat (TAK-924);Pevonedistat, 10 mM in DMSO;Pevonedistat (MLN-4924,TAK 924)
- CBNumber:
- CB92510096
- Summenformel:
- C21H25N5O4S
- Molgewicht:
- 443.52
- MOL-Datei:
- 905579-51-3.mol
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Pevonedistat Eigenschaften
- Schmelzpunkt:
- 161-163°C
- Siedepunkt:
- 721.0±70.0 °C(Predicted)
- Dichte
- 1.62
- storage temp.
- -20°C Freezer
- L?slichkeit
- Soluble in DMSO (up to 10 mg/ml).
- Aggregatzustand
- solid
- pka
- 9.35±0.70(Predicted)
- Farbe
- White
- Stabilit?t:
- Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.
- InChIKey
- MPUQHZXIXSTTDU-QXGSTGNESA-N
- SMILES
- S(N)(OC[C@@H]1C[C@@H](N2C3C(C=C2)=C(N[C@@H]2C4=C(C=CC=C4)CC2)N=CN=3)C[C@@H]1O)(=O)=O
Sicherheit
- Risiko- und Sicherheitserkl?rung
- Gefahreninformationscode (GHS)
| Bildanzeige (GHS) |
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| Alarmwort |
Warnung |
| Gefahrenhinweise |
| Code |
Gefahrenhinweise |
Gefahrenklasse |
Abteilung |
Alarmwort |
Symbol |
P-Code |
| H315 |
Verursacht Hautreizungen. |
Hautreizung |
Kategorie 2 |
Warnung |
![GHS hazard pictograms]() src="/GHS07.jpg" width="20" height="20" /> |
P264, P280, P302+P352, P321,P332+P313, P362 |
| H319 |
Verursacht schwere Augenreizung. |
Schwere Augenreizung |
Kategorie 2 |
Warnung |
![GHS hazard pictograms]() src="/GHS07.jpg" width="20" height="20" /> |
P264, P280, P305+P351+P338,P337+P313P |
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| Sicherheit |
| P264 |
Nach Gebrauch gründlich waschen. |
| P264 |
Nach Gebrauch gründlich waschen. |
| P280 |
Schutzhandschuhe/Schutzkleidung/Augenschutz tragen. |
| P302+P352 |
BEI BERüHRUNG MIT DER HAUT: Mit viel Wasser/... (Hersteller kann, falls zweckm??ig, ein Reinigungsmittel angeben oder, wenn Wasser eindeutig ungeeignet ist, ein alternatives Mittel empfehlen) waschen. |
| P305+P351+P338 |
BEI KONTAKT MIT DEN AUGEN: Einige Minuten lang behutsam mit Wasser spülen. Eventuell vorhandene Kontaktlinsen nach M?glichkeit entfernen. Weiter spülen. |
| P332+P313 |
Bei Hautreizung: ?rztlichen Rat einholen/?rztliche Hilfe hinzuziehen. |
| P337+P313 |
Bei anhaltender Augenreizung: ?rztlichen Rat einholen/?rztliche Hilfe hinzuziehen. |
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Pevonedistat Chemische Eigenschaften,Einsatz,Produktion Methoden
Chemische Eigenschaften
White Solid
Enzyminhibitor
This first-in-class small molecule inhibitor (FW = 443.52 g/mol; CAS 905579-51-3; Solubility = 10 mg/mL DMSO), also named MLN4924 and [(1S,2S,4R)-4-[4-[[(1S)-2,3-dihydro-1H-inden-1-yl]amino]-7H-pyrrolo[2,3- d]pyrimidin-7-yl]-2-hydroxycyclopentyl]sulfamate methyl ester, targets Nedd8 activating enzyme, or NAE (IC50 = 4.7 nM), with much weaker action against UAE (IC50 = 1.5 μM), SAE (IC50 = 8.2 μM), and UBA6 (IC50 = 1.8 μM). In most cancer cells, pevonedistat treatment results in the induction of DNA re-replication, resulting in DNA damage and cell death. MLN4924 also exhibits an alternative mechanism of action. Treatment of activated B cell-like (ABC) diffuse large B-cell lymphoma (DLBCL) cells with pevonedistat resulted in rapid accumulation of pIkBa, decrease in nuclear p65 content, reduction of transcriptional activity of NF-kB (or nuclear factor k-light-chain-enhancer of activated B cells), and G1 arrest, ultimately resulting in apoptosis induction, events consistent with potent NF-kB pathway inhibition. Treatment of germinal-center B cell-like (GCB) DLBCL cells resulted in an increase in cellular Cdt-1 and accumulation of cells in S-phase, consistent with cells undergoing DNA rereplication. Pevonedistat also inhibits Vpx/Vpr-induced SAMHD1 degradation by inhibiting the neddylation of E3 ubiquitin-ligase and blocking SIVmac replication in myeloid cells, therebyindicating the potential efficacy of inhibiting neddylation as an antiretroviral strategy
Pevonedistat Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
Pevonedistat Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.
Global( 163)Lieferanten
905579-51-3()Verwandte Suche:
- ((1S,2S,4R)-4-(4-(((S)-2,3-dihydro-1H-inden-1-yl)aMino)-7H-pyrrolo[2,3-d]pyriMidin-7-yl)-2-hydroxycyclopentyl)Methyl sulfaMate
- [(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 sulfaMate
- Pevonedistat
- MLN4924 (Pevonedistat)
- Sulfamic acid [(1S,2S,4R)-4-[4-[[(1S)-2,3-dihydro-1H-inden-1-yl]amino]-7H-pyrrolo[2,3-d]pyrimi
- 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
- CS-821
- TAK-924
- PEVONEDISTAT;MLN-4924
- mln4924 Free Base
- Pevonedistat (MLN-4924,TAK 924)
- ((1S,2S,4S)-4-(4-(((S)-2,3-dihydro-1H-inden-1-yl)amino)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-2-hydroxycyclopentyl)methyl sulfamate
- (1S,2S,4R)-4-[4-[[(1S)-2,3-dihydro-1H-inden-1-yl]amino]pyrrolo[2,3-d]pyrimidin-7-yl]-2-hydroxycyclopentyl]methyl sulfamate
- Pevonedistat (TAK-924)
- Pevonedistat ISO 9001：2015 REACH
- MLN 4924
- MLN-4924, NEDD8-activating enzyme inhibitor
- Pevonedistat, 10 mM in DMSO
- 905579-51-3
- C21H25N5O4S
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