AZD-9291
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- CAS-Nr.
- 1421373-65-0
- Englisch Name:
- AZD-9291
- Synonyma:
- Mereletinib;N-(2-{2-dimethylaminoethyl-methylamino}-4-methoxy-5-{[4-(1-methylindol-3-yl)pyrimidin-2-yl]amino}phenyl)prop-2-enamide;ZAD9291;Osimertinib Intermediate 4;N-(2-{[2-(Dimethylamino)ethyl](methyl)amino}-4-methoxy-5-{[4-(1-methyl-1H-indol-3-yl)pyrimidin;osim;CS-943;ADZ9291;Ochinib;AZD-9291
- CBNumber:
- CB02677059
- Summenformel:
- C28H33N7O2
- Molgewicht:
- 499.61
- MOL-Datei:
- 1421373-65-0.mol
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AZD-9291 Eigenschaften
- Schmelzpunkt:
- >188oC (dec.)
- Dichte
- 1.19±0.1 g/cm3(Predicted)
- storage temp.
- Hygroscopic, -20°C Freezer, Under inert atmosphere
- L?slichkeit
- DMSO (Slightly, Heated), Methanol (Slightly, Heated)
- pka
- 12.68±0.70(Predicted)
- Aggregatzustand
- Solid
- Farbe
- Pale Yellow to Beige
- CAS Datenbank
- 1421373-65-0
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 |
| H335 |
Kann die Atemwege reizen. |
Spezifische Zielorgan-Toxizit?t (einmalige Exposition) |
Kategorie 3 (Atemwegsreizung) |
Warnung |
![GHS hazard pictograms]() src="/GHS07.jpg" width="20" height="20" /> |
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| Sicherheit |
| P261 |
Einatmen von Staub vermeiden. |
| P264 |
Nach Gebrauch gründlich waschen. |
| P264 |
Nach Gebrauch gründlich waschen. |
| P271 |
Nur im Freien oder in gut belüfteten R?umen verwenden. |
| 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. |
| P304+P340 |
BEI EINATMEN: Die Person an die frische Luft bringen und für ungehinderte Atmung sorgen. |
| P305+P351+P338 |
BEI KONTAKT MIT DEN AUGEN: Einige Minuten lang behutsam mit Wasser spülen. Eventuell vorhandene Kontaktlinsen nach M?glichkeit entfernen. Weiter spülen. |
| P312 |
Bei Unwohlsein GIFTINFORMATIONSZENTRUM/Arzt/... (geeignete Stelle für medizinische Notfallversorgung vom Hersteller/Lieferanten anzugeben) anrufen. |
| P321 |
Besondere Behandlung |
| 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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AZD-9291 Chemische Eigenschaften,Einsatz,Produktion Methoden
Beschreibung
AZD-9291 (Mesylate), also known as Osimertinib, belongs to a third-generation EGFR (epidermal growth factor receptor) inhibitor. It can be used for the treatment of locally advanced or metastatic non-small cell lung cancer (NSCLC) in case when the cancer cells carry specific mutations (such as T790M) in the epidermal growth factor receptor. It takes effect through directly binding to the certain mutant forms of EGFR (T790M, L858R, and exon 19 deletions) that are frequently found in NSCLC, further causing poor prognosis for late-stage disease. Since it spares wild type EGFR during therapy, it has only limited toxicity.
Verwenden
AZD 9291 is an irreversible inhibitor of epidermal growth factor receptor (EGFR) sensitizing and T790M resistance mutations (IC50s = 15-17 nM) while sparing the wild-type form of the receptor (IC50 = 480 nM). It binds the related IGF1R and hERG receptors with significantly reduced potency (IC50s = 2.9 and 16.2 μM, respectively). AZD 9291 has been shown to inhibit tumor growth in a xenograft mouse model at oral doses of 5-10 mg/kg and has been tested clinically in patients with advanced EGFR mutant non-small-cell lung cancer.[Cayman Chemical]
Indications
The collection of ibrutinib (Imbruvica(R), Pharmacyclics Inc.), afatinib, and osimertinib represents the small, yet expanding, group of covalent SMKIs. Ibrutinib is a non-receptor Bruton’s tyrosine kinase inhibitor approved for the treatment of relapsed chronic lymphocytic leukemia. Afatinib, approved for NSCLC in 2013 and squamous NSCLC in 2016, is a second-generation irreversible EGFR inhibitor that targets wild-type EGFR, the mutant T790M EGFR, and HER2. Osimertinib (AZD9291), which was approved by FDA in November 2015, is a third-generation irreversible EGFR inhibitor that selectively targets the mutant T790M EGFR. Rociletinib, which shares a high degree of structural similarity with that of osimertinib, is a promising covalent EGFR inhibitor developed by Clovis Oncology aimed for the treatment of patients with EGFR T790M-mutated NSCLC, until the company terminated its development in May 2016 following a negative vote fromthe FDA’sOncologic Drugs Advisory Committee.
Definition
ChEBI: A member of the class of aminopyrimidines that is 4-(1-methylindol-3-yl)pyrimidin-2-amine in which one of the amino hydrogens is replaced by a 2-methoxy-4-[2-(dimethylamino)ethyl](methyl)amino-5-acrylamidophenyl group. Used (as the mesylate salt) for treat
ent of EGFR T790M mutation positive non-small cell lung cancer.
Einzelnachweise
http://www.medkoo.com/products/6711
https://en.wikipedia.org/wiki/Osimertinib
https://www.drugbank.ca/drugs/DB09330
AZD-9291 Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
AZD-9291 Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.
Global( 386)Lieferanten
1421373-65-0()Verwandte Suche:
- N-(2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxy-5-((4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl)amino)phenyl)acrylamide
- Mereletinib mesylate(AZD9291)
- AZD9291 (free base)
- Osimertinib (AZD-9291)
- AZD9291, Osimertinib
- AZD9291 Base
- Osimertinib Base
- AZD9291 10G
- AZD-9291
- N(2{[2(diMethylaMino)ethyl](Methyl)aMino}4Methoxy5{[4(1Methyl1Hindol3yl)pyriMidin2yl]aMino}phenyl)prop2enaMide
- N-[2-[[2-(Dimethylamino)ethyl]methylamino]-4-methoxy-5-[[4-(1-methyl-1H-indol-3-yl)-2-pyrimidinyl]amino]phenyl]-2-propenamide
- AZD9291,AZD-9291
- 2-Propenamide, N-[2-[[2-(dimethylamino)ethyl]methylamino]-4-methoxy-5-[[4-(1-methyl-1H-indol-3-yl)-2-pyrimidinyl]amino]phenyl]-
- AZD9291 N-[2-[[2-(Dimethylamino)ethyl]methylamino]-4-methoxy-5-[[4-(1-methyl-1H-indol-3-yl)-2-pyrimidinyl]amino]phenyl]-2-propenamide
- N-[2-[[2-(Dimethylamino)ethyl]methylamino]-4-methoxy-5-[[4-(1-methyl-1H-indol-3-yl)-2-pyrimidinyl]amino]phenyl]-2-propenamide AZD9291
- AZD9291, >=98%
- AZD929/Osimertinib
- Osimertinib, 98%, a potent and selective mutated forms EGFR inhibitor
- Pharmaceutical Chemical Anticancer Drug Azd-9291 for for Lung Cancer 1421373-65-0
- N1-[2-(Dimethylamino)ethyl]-2-methoxy-N1-methyl-N4-[4-(1-methyl-1H-indol-3-yl)-2-pyrimidinyl]-1,4-benzenetriamine
- AZD-92941
- CS-943
- ADZ9291
- Mereletinib(AZD-9291,Osimertinib)
- EGFR INHIBITOR; AZD9291; AZD 9291;TAGRISSO
- osim
- EGFR INHIBITOR;AZD9291;AZD 9291;TAGRISSO;OSIMERTINIB;MERELETINIB
- Ochinib
- N-(2-{2-dimethylaminoethyl-methylamino}-4-methoxy-5-{4-(1-methylindol-3-yl)pyrimidin-2-yl}amino}phenyl)prop-2enamide (AZD9291 free base)
- )amino)-4-methoxy-5-((4-(1-methyL
- N-(2-((2-(DimethyL
- AZD-9291 USP/EP/BP
- N-(2-{2-dimethylaminoethyl-methylamino}-4-methoxy-5-{[4-(1-methylindol-3-yl)pyrimidin-2-yl]amino}phenyl)prop-2-enamide
- Mereletinib
- ZAD9291
- N-(2-{[2-(Dimethylamino)ethyl](methyl)amino}-4-methoxy-5-{[4-(1-methyl-1H-indol-3-yl)pyrimidin
- Osimertinib Intermediate 4
- Ethanone,1-[5-bromo-3-(trifluoromethyl)-6-pyridinyl]-
- 13C,2H3]-Osimertinib
- Osimeitinib
- Meritinib
- Ostinidine
- Ostinib (AZD9291)
- 1421373-65-0
- 421373-65-0
- 1421273-65-0
- C28H33N7O2
- Inhibitors
- API
- Anticancer
- AZD9291
- 1421373-65-0
