MLN9708
|
|
|
- CAS-Nr.
- 1201902-80-8
- Englisch Name:
- MLN9708
- Synonyma:
- MLN9708;CS-1830;Ninlaro);MLN-9708 analog;MLN 9708 analog;MLN9708;MLN-9708;Ixazomib Citrate;Esazomide citrate;MLN9708,MLN-9708,MLN 9708;MLN 9708 - Ixazomib citrate
- CBNumber:
- CB82521079
- Summenformel:
- C20H23BCl2N2O9
- Molgewicht:
- 517.12
- MOL-Datei:
- 1201902-80-8.mol
|
MLN9708 Eigenschaften
- Schmelzpunkt:
- >227°C (dec.)
- Dichte
- 1.47
- storage temp.
- Hygroscopic, -20°C Freezer, Under inert atmosphere
- Löslichkeit
- DMSO (Slightly), Methanol (Slightly, Heated, Sonicated)
- pka
- 1.92±0.20(Predicted)
- Aggregatzustand
- Solid
- Farbe
- White to Off-White
Sicherheit
- Risiko- und Sicherheitserklärung
- Gefahreninformationscode (GHS)
| S-Sätze: |
24/25 |
|
|
| HS Code |
29329990 |
|
|
| Bildanzeige (GHS) |
|
| Alarmwort |
Warnung |
| Gefahrenhinweise |
| Code |
Gefahrenhinweise |
Gefahrenklasse |
Abteilung |
Alarmwort |
Symbol |
P-Code |
| H302 |
Gesundheitsschädlich bei Verschlucken. |
Akute Toxizität oral |
Kategorie 4 |
Warnung |
![GHS hazard pictograms]() src="/GHS07.jpg" width="20" height="20" /> |
P264, P270, P301+P312, P330, P501 |
| 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 |
| H335 |
Kann die Atemwege reizen. |
Spezifische Zielorgan-Toxizität (einmalige Exposition) |
Kategorie 3 (Atemwegsreizung) |
Warnung |
![GHS hazard pictograms]() src="/GHS07.jpg" width="20" height="20" /> |
|
|
| Sicherheit |
| P261 |
Einatmen von Staub vermeiden. |
| P305+P351+P338 |
BEI KONTAKT MIT DEN AUGEN: Einige Minuten lang behutsam mit Wasser spülen. Eventuell vorhandene Kontaktlinsen nach Möglichkeit entfernen. Weiter spülen. |
|
MLN9708 Chemische Eigenschaften,Einsatz,Produktion Methoden
Beschreibung
Ixazomib citrate is a
proteasome inhibitor prodrug for the treatment of multiple
myeloma in patients who have received at least one prior
therapy in combination with lenalidomide and dexamethasone. The drug was developed by Takeda and reversibly
inhibits the protein proteasome subunit β type-5, which is part
of the 20S proteasome complex. Ixazomib citrate (XXIV) is
hydrolyzed quickly in vivo to give the biologically active
compound ixazomib, which presumably is the corresponding
boronic acid variant of XXIV.
Verwenden
MLN-9708 is a novel proteasome?inhibitor.
Synthese
The structure of ixazomib citrate is particularly interesting in
that it is one of the relatively few marketed drugs which feature
a boron atom within its structure (others of note being the
oncology medication bortezomib and the antifungal drug
tavaborole13). The ostensible scale synthetic approach began
with reaction of commercial 2,5-dichlorobenzoyl chloride (188) with glycine in aqueous NaOH to furnish amide
189 in 97% yield as a white crystalline solid. Acid 189 was then
coupled with commercially available 1,3,2-benzodioxaborolane
190 in the presence of TBTU and DIPEA in DMF at low
temperature to give diamide 191, which was used without
purification for the next step. Borane 191 was then deprotected
with (2-methylpropyl)boronic acid in methanolic HCl to
provide trimer 192 in 74% as a white solid. Finally, boroxin
192 was reacted with citric acid in EtOAc to dissociate the
trimer, resulting in ixazomib citrate (XXIV) in 88% yield as a
crystalline solid.
MLN9708 Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
MLN9708 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.
Global( 182)Lieferanten
1201902-80-8()Verwandte Suche:
- 4-(carboxymethyl)-2-((R)-1-(2-(2,5-dichlorobenzamido)acetamido)-3-methylbutyl)-6-oxo-1,3,2-dioxaborinane-4-carboxylic acid
- MLN9708
- MLN9708,MLN-9708,MLN 9708
- 4-Carboxy-2-[(1R)-1-[[2-[(2,5-dichlorobenzoyl)amino]acetyl]amino]-3-methylbutyl]-6-oxo-1,3,2-dioxaborinane-4-acetic acid
- 4-Carboxy-2-[(1R)-1-[[2-[(2,5-dichlorobenzoyl)amino]acetyl]amino]-3-methylbutyl]-6-oxo-1,3,2-dioxaborinane-4-acetic acid MLN9708
- Ixazomib Citrate
- MLN9708;MLN-9708
- 4-(Carboxymethyl)-2-((R)-1-(2-(2,5-dichlorobenzamido)acetamido)-3-methylbutyl)-6-oxo-1,3,2-dio
- MLN 9708 analog
- MLN-9708 analog
- 4-(carboxymethyl)-2-(1-(2-(2,5-dichlorobenzamido)acetamido)-3-methylbutyl)-6-oxo-1,3,2-dioxaborinane-4-carboxylic acid
- MLN 9708 - Ixazomib citrate
- CS-1830
- MLN9708, 98%, 20S proteasome inhibitor
- 1,3,2-Dioxaborinane-4-acetic acid, 4-carboxy-2-[(1R)-1-[[2-[(2,5-dichlorobenzoyl)amino]acetyl]amino]-3-methylbutyl]-6-oxo-
- Ninlaro)
- Esazomide citrate
- Ixazomib Citrate (MLN9708) Analogue
- 1201902-80-8
- C20H23BCl2N2O9
- Inhibitors
- Inhibitor
- Apis
