Gefitinib
|
|
|
- CAS-Nr.
- 184475-35-2
- Englisch Name:
- Gefitinib
- Synonyma:
- Gefinitib;Gifitinib;Gefltinib;Gefitinib Tablets;N-(3-Chloro-4-fluorophenyl)-7-methoxy-6-[3-(4-morpholinyl)propoxy]-4-quinazolinamine;N-(3-Chlor-4-fluorophenyl)-7-[methoxy-6-[(3-morpholin-4-yl)propoxyl]-quinazolin-4-yl]amine;ressa;CS-524;ZD 1839;efitinib
- CBNumber:
- CB8120056
- Summenformel:
- C22H24ClFN4O3
- Molgewicht:
- 446.9
- MOL-Datei:
- 184475-35-2.mol
|
Gefitinib Eigenschaften
- Schmelzpunkt:
- 119-1200C
- Siedepunkt:
- 586.8±50.0 °C(Predicted)
- Dichte
- 1.322±0.06 g/cm3(Predicted)
- storage temp.
- room temp
- L?slichkeit
- Soluble in DMSO (up to 40 mg/ml) or in Ethanol (up to 4 mg/ml).
- pka
- 7.00±0.10(Predicted)
- Aggregatzustand
- powder
- Farbe
- white to beige
- Stabilit?t:
- Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 1 month.
- InChI
- InChI=1S/C22H24ClFN4O3/c1-29-20-13-19-16(12-21(20)31-8-2-5-28-6-9-30-10-7-28)22(26-14-25-19)27-15-3-4-18(24)17(23)11-15/h3-4,11-14H,2,5-10H2,1H3,(H,25,26,27)
- InChIKey
- XGALLCVXEZPNRQ-UHFFFAOYSA-N
- SMILES
- N1=C2C(C=C(OCCCN3CCOCC3)C(OC)=C2)=C(NC2=CC=C(F)C(Cl)=C2)N=C1
- CAS Datenbank
- 184475-35-2(CAS DataBase Reference)
Sicherheit
- Risiko- und Sicherheitserkl?rung
- Gefahreninformationscode (GHS)
| S-S?tze: |
24/25 |
|
|
| WGK Germany |
WGK 3 |
|
|
| HS Code |
29349990 |
|
|
| Speicherklasse |
6.1C - Combustible acute toxic Cat.3
toxic compounds or compounds which causing chronic effects |
|
|
| Hazard Classifications |
Acute Tox. 4 Oral
Aquatic Chronic 1
Carc. 2
Eye Dam. 1
Repr. 1B
Skin Irrit. 2
STOT RE 2 Oral |
|
|
| Bildanzeige (GHS) |
|
| Alarmwort |
Warnung
|
| Gefahrenhinweise |
| Code |
Gefahrenhinweise |
Gefahrenklasse |
Abteilung |
Alarmwort |
Symbol |
P-Code |
| H302 |
Gesundheitssch?dlich bei Verschlucken. |
Akute Toxizit?t oral |
Kategorie 4 |
Warnung |
|
P264, P270, P301+P312, P330, P501 |
| H315 |
Verursacht Hautreizungen. |
Hautreizung |
Kategorie 2 |
Warnung |
|
P264, P280, P302+P352, P321,P332+P313, P362 |
| H319 |
Verursacht schwere Augenreizung. |
Schwere Augenreizung |
Kategorie 2 |
Warnung |
|
P264, P280, P305+P351+P338,P337+P313P |
| H335 |
Kann die Atemwege reizen. |
Spezifische Zielorgan-Toxizit?t (einmalige Exposition) |
Kategorie 3 (Atemwegsreizung) |
Warnung |
|
|
|
| Sicherheit |
| P305+P351+P338 |
BEI KONTAKT MIT DEN AUGEN: Einige Minuten lang behutsam mit Wasser spülen. Eventuell vorhandene Kontaktlinsen nach M?glichkeit entfernen. Weiter spülen. |
|
Gefitinib Chemische Eigenschaften,Einsatz,Produktion Methoden
Beschreibung
Gefitinib was introduced in Japan as a daily oral monotherapy for the treatment of
inoperable or recurrent non-small cell lung cancers (NSCLC). This
inhibits autophosphorylation of EGRF and blocks the cascade of intracellular events which
have been implicated in the proliferation, survival and metastasis of cancer cells.
Chemische Eigenschaften
Light-Yellow Crystalline Powder
Indications
The EGFR or ErbB1 inhibitor gefitinib (Iressa(R), AstraZeneca) was originally approved by the US FDA in 2003 under accelerated regulations for the treatment of locally advanced or metastatic non-small cell lung cancer (NSCLC) after progression on docetaxel- and platinum-based chemotherapy.
Allgemeine Beschreibung
Geftinib is available as 250-mg tablets for oral administrationin the treatment of NSCLC for those patients who have failedto respond to platinum-based therapies and docetaxel and hasalso been used against squamous cell cancers of the head andneck. The agent is an inhibitor of the TK of EGF-R and possiblyother TKs as well. Gefitinib is both a substrate and inhibitorof Pgp and BCRP. The agent is absorbed slowly afterbeing administered orally with 60% bioavailability.Metabolism occurs in the liver and is mediated primarily byCYP3A4 to give eight identified metabolites resulting fromdefluorination of the phenyl ring, oxidative-O-demethylation,and multiple products arising as a result of oxidation of themorpholine ring. The O-demethylated product represents thepredominate metabolite and is 14-fold less active comparedwith the parent. The parent and metabolites are eliminated inthe feces with a terminal elimination half-life of 48 hours.The drug appears to be well tolerated with the most commonlyreported side effects being rash and diarrhea. It mayalso cause elevations in blood pressure especially in those patientswith preexisting hypertension, elevation of transaminaselevels, and mild nausea and mucositits.
Allgemeine Beschreibung
Class: receptor tyrosine kinase
Treatment: NSCLC
Oral bioavailability = 60%
Elimination half-life = 48 h
Protein binding = 97%
Biologische Aktivit?t
Orally active, selective inhibitor of EGFR tyrosine kinase (IC 50 = 23-79 nM). Shows minimal activity against ErbB2, KDR, c-flt, PKC, MEK and ERK-2. Blocks EGFR autophosphorylation and inhibits tumor growth in mice bearing a range of human xenografts.
Gefitinib Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
Gefitinib Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.
Global( 818)Lieferanten
184475-35-2()Verwandte Suche:
- N-(3-Chloro-4-fluoro-phenyl)-7-methoxy-6-(3-morpholin-4-ylpropoxy)quinazolin-4-amine Gefitinib
- Gefitinib, >=99%
- GEFITINIB RELATED COMPOUND
- Gefitinib
N-(3-Chloro-4-fluoro-phenyl)-7-methoxy-6-(3-morpholin-4-ylpropoxy)quinazolin-4-amine
- GEFITINIB
- n-(3-chloro-4-fluoro-phenyl)-7-methoxy-6-(3-morpholin-4-ylpropoxy)quinazolin-4-amine
- ZD 1839
- 4-Quinazolinamine, N-(3-chloro-4-fluorophenyl)-7-methoxy-6-[3-(4-morpholinyl)propoxy]-
- AKOS 91371
- Gefitinib(TINIBS)
- 6-(Benzyloxy)-7-methoxyquinazolin-4(3H)-one
- (3-chloro-4-fluoro-phenyl)-[7-methoxy-6-(3-morpholinopropoxy)quinazolin-4-yl]amine
- N-(4-bromo-2-fluorophenyl)-7-methoxy-6-(3-morpholinopropoxy)quinazolin-4-amine
- Gefitinib, Iressa, ZD1839
- ZD1839; IRESSA
- Getfitnib
- N-(3-Chloro-4-fluorophenyl)-7-Methoxy-6-(3-Morpholinopropoxy)quinazolin-4-aMine
- Gefitinib (ZD1839)
- Gefitinib WS
- Gefitinib(AZ-1839)
- CS-524
- Gefitinib (ZD1839, Iressa)
- N-(3-chloro-4-fluorophenyl)-7-methoxy
- ZD-1839;ZD 1839
- Gefitinib for system suitability CRS
- efitinib
- Gefitinib for system suitability
- Iressa Gefitinib
- Gefitinib USP/EP/BP
- gefitinib high quali
- Gefitinib (API)
- Gefitinib（USFDA/CEP）
- Anti-cancer pharmaceutical Gefitinib
- Gefitinib for system suitability (Y0001809)Q: What is
Gefitinib for system suitability (Y0001809) Q: What is the CAS Number of
Gefitinib for system suitability (Y0001809)
- GefitinibQ: What is
Gefitinib Q: What is the CAS Number of
Gefitinib Q: What is the storage condition of
Gefitinib Q: What are the applications of
Gefitinib
- Ji Fei Ji
- 4-[(3-Chloro-4-fluorophenyl)amino]-7-methoxy-6-(3-morpholinopropoxy)quinazoline
- Gefitinib 184475-35-2
- N-(3-Chlor-4-fluorophenyl)-7-[methoxy-6-[(3-morpholin-4-yl)propoxyl]-quinazolin-4-yl]amine
- N-(3-Chloro-4-fluorophenyl)-7-methoxy-6-[3-(4-morpholinyl)propoxy]-4-quinazolinamine
- Gefinitib
- Gifitinib
- Gefitinib Tablets
- Benzenamine,2-bromo-9-methyl-
- EGFR tyrosine kinase,Autophagy,lung cancer,breast cancer,Gefitinib,phosphorylation,Inhibitor,ZD 1839,Apoptosis,inhibit,TAMs,NSCLCs,EGFR,ZD-1839,antitumour,Epidermal growth factor receptor,HER1,tumor metastasis,ErbB-1
- GEFITINIB BP -2 KG
- Gefitinib, EGFR tyrosine kinase inhibitor
- Gefitinib, 10 mM in DMSO
- Gefitinib - Bio-X ?
- Gefitinib RS
- N-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-morpholine-4-propoxy)quinolineazoleline-4-amine
- ressa
- Gefitinib (Standard)
- Gefltinib
- 184475-35-2
- 1884475-35-2
- 84475-35-2
- C22H24ClFN4O3
