Lapatinib
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- CAS-Nr.
- 231277-92-2
- Englisch Name:
- Lapatinib
- Synonyma:
- Tykerb;Tyverb;CS-220;GW-2016;CS-1860;GW 57201;Rapatini;lapatinib;GSK572016;GW-572016
- CBNumber:
- CB8855402
- Summenformel:
- C29H26ClFN4O4S
- Molgewicht:
- 581.06
- MOL-Datei:
- 231277-92-2.mol
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Lapatinib Eigenschaften
- Schmelzpunkt:
- 144-146oC
- Siedepunkt:
- 750.7±60.0 °C(Predicted)
- Dichte
- 1.381±0.06 g/cm3(Predicted)
- storage temp.
- 2-8°C(protect from light)
- L?slichkeit
- Soluble in DMSO (up to 200 mg/ml)
- Aggregatzustand
- solid
- pka
- 6.34±0.19(Predicted)
- Farbe
- Yellow
- Stabilit?t:
- Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.
- InChIKey
- BCFGMOOMADDAQU-UHFFFAOYSA-N
- SMILES
- N1=C2C(C=C(C3=CC=C(CNCCS(C)(=O)=O)O3)C=C2)=C(NC2=CC=C(OCC3=CC=CC(F)=C3)C(Cl)=C2)N=C1
- CAS Datenbank
- 231277-92-2(CAS DataBase Reference)
Sicherheit
- Risiko- und Sicherheitserkl?rung
- Gefahreninformationscode (GHS)
| Bildanzeige (GHS) |
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| Alarmwort |
Warnung |
| Gefahrenhinweise |
| Code |
Gefahrenhinweise |
Gefahrenklasse |
Abteilung |
Alarmwort |
Symbol |
P-Code |
| 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 |
| H362 |
Kann S?uglinge über die Muttermilch sch?digen. |
Reproductive toxicity, effects on or via lactation |
Additional category |
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P201, P260, P263, P264, P270,P308+P313 |
| H413 |
Kann für Wasserorganismen sch?dlich sein, mit langfristiger Wirkung. |
Langfristig (chronisch) gew?ssergef?hrdend |
Kategorie 4 |
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| Sicherheit |
| P201 |
Vor Gebrauch besondere Anweisungen einholen. |
| P260 |
Dampf/Aerosol/Nebel nicht einatmen. |
| P263 |
Kontakt w?hrend der Schwangerschaft /und der Stillzeit vermeiden. |
| P273 |
Freisetzung in die Umwelt vermeiden. |
| P305+P351+P338 |
BEI KONTAKT MIT DEN AUGEN: Einige Minuten lang behutsam mit Wasser spülen. Eventuell vorhandene Kontaktlinsen nach M?glichkeit entfernen. Weiter spülen. |
| P308+P313 |
BEI Exposition oder falls betroffen: ?rztlichen Rat einholen/?rztliche Hilfe hinzuziehen. |
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Lapatinib Chemische Eigenschaften,Einsatz,Produktion Methoden
Beschreibung
Lapatinib, a new member of the 4-anilinoquinazoline class of RTK inhibitors
(RTKIs), was launched as an oral treatment for breast cancer.
Lapatinib has dual affinity for EGFR and HER2 tyrosine kinases. It is indicated
in combination with capecitabine for treating patients with advanced or
metastatic breast cancer whose tumors overexpress HER2 and who have
received prior therapy including an anthracycline, a taxane, and trastuzumab.
Previously marketed drugs from the 4-anilinoquinazoline class include
erlotinib (Tarceva) and gefitinib (Iressa
TM), both of which are indicated for
treating non-small-cell lung cancer (NSCLC). As with erlotinib and gefitinib, To Market, To Market 2007 475 lapatinib is an ATP-competitive kinase inhibitor. It inhibits the tyrosine kinase activity EGFR and HER-2 with apparent Ki values of 3 and 13 nM, respectively, and has slow off-rate kinetics (t1/2X300 min).
In addition, dividing the daily dose of lapatinib results in approximately 2-fold higher exposure at steady state compared to the same total dose administered once daily.
The chemical synthesis of lapatinib entails the condensation of 4-chloro-6-iodoquinazoline and 3-chloro-4-(3-fluorobenzyloxy)aniline to produce a diaryl amine intermediate followed by Stille coupling of the iodo group with 5-dioxolanyl-2-(tributylstannyl)furan and subsequent acid hydrolysis of the cyclic ketal to the corresponding aldehyde. Finally, reductive amination of the aldehyde intermediate with 2-(methanesulfonyl) ethylamine in the presence of sodium triacetoxyborohydride produces lapatinib.
.
Allgemeine Beschreibung
Class: receptor tyrosine kinase
Treatment: HER2-positive breast cancer
Elimination half-life = 24 h
Protein binding = 99%
Lapatinib Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
Lapatinib Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.
Global( 533)Lieferanten
231277-92-2()Verwandte Suche:
- lapatinib
- n-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[(2-methylsulfonylethylamino)methyl]-2-furyl]quinazolin-4-amine
- 4-Quinazolinamine, N-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[[[2-(methylsulfonyl)ethyl]amino]methyl]-2-furanyl]-
- Lapatinib(TINIBS)
- Lapatinib Base N-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[[[2-(methylsulfonyl)ethyl]amino]methyl]-2-furanyl]-4-Quinazolinamine
- GW2016 LAPATINIB
- N-(3-chloro-4-((3-fluorobenzyl)oxy)phenyl)-6-(5-(((2-(methylsulfonyl)ethyl)amino)methyl)furan-2-yl)quinazolin-4-amine
- N-{3-chloro-4-[(3-fluorobenzyl)oxyl]phenyl}-6-[5-({[2-(methylsulfonyl)ethyl]amino}methyl)furan-2-yl]quinazolin-4-amine
- GW-2016
- Tyverb 4-[[3-Chloro-4-(3-fluorobenzyloxy)phenyl]aMino]-6-[5-[[(2-Methanesulfonylethyl)aMino]Methyl]furan-2-yl]quinazoline
- Lapatinib Ditosylate (API)
- 4-[[3-Chloro-4-(3-fluorobenzyloxy)phenyl]amino]-6-[5-[[(2-methanesulfonylethyl)amino]methyl]furan-2-yl]quinazoline
- GSK572016
- GW 57201
- N-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[[[2-(methylsulfonyl)ethyl]amino]methyl]-2-furanyl]-4-quinazolinamine
- N-{3-chloro-4-[(3-fluorophenyl)Methoxy]phenyl}-6-(5-{[(2-Methanesulfonylethyl)aMino]Methyl}furan-2-yl)quinazolin-4-aMine
- N-{3-Chloro-4-[(3-fluorobenzyl)oxy]phenyl}-6-[5-({[2-(Methanesulphonyl)ethyl]aMino}Methyl)-furan-2-yl]-4-quinazolinaMine
- Lapatinib (2TsOH)
- Lapatinib, 99+%
- GW-572016
- GW-572016; TYKERB
- Lapatinib free base
- Lapatinib(GSK572016)
- Lapatinib N-[3-Chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[(2-methylsulfonylethylamino)methyl]-2-furyl]quinazolin-4-amine
- N-[3-Chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[(2-methylsulfonylethylamino)methyl]-2-furyl]quinazolin-4-amine Lapatinib
- Lapatinib(ditosylate salt)
- GW572016;GW-572016;GW 572016
- CS-220
- Lapatinib (GW572016, Tykerb)
- CS-1860
- N-[3-Chloro-4-[(3-fluorobenzyl)oxy]phenyl]-6-[5-[[[2-(methylsulfonyl)ethyl]amino]methyl]-2-furyl]-4-quinazolinamine
- Lapatinib USP/EP/BP
- Lapatinib (GW-572016, Tykerb, Tyverb)
- N-[3-Chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[(2-methylsulfonylethylamino)methyl]-2-furyl]quinazolin-4-amine
- LapatinibQ: What is
Lapatinib Q: What is the CAS Number of
Lapatinib Q: What is the storage condition of
Lapatinib Q: What are the applications of
Lapatinib
- TIANFUCHEM--231277-92-2-- Lapatinib in stock
- Tykerb
- Tyverb
- 1,10-Phenanthroline-5,10-dione
- Rapatini
- Rapatinib base
- 2H4]-Lapatinib
- 231277-92-2
- 31277-92-2
- C29H26ClFN4O4S
- Inhibitors
- Anti-cancer&immunity
- Lapatinib
- APIs
- API
- Pharmaceutical intermediate
- anti-neoplastic
- Molecular Targeted Antineoplastic
- 231277-92-2
