Encorafenib (LGX818)
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- CAS-Nr.
- 1269440-17-6
- Englisch Name:
- Encorafenib (LGX818)
- Synonyma:
- Encorafenib;LGX818;LGX-818;(S)-Methyl [1-[[4-[3-[5-chloro-2-fluoro-3-(methylsulfonamido)phenyl]-1-isopropyl-1H-pyrazol-4-yl]pyrimidin-2-yl]amino]propan-2-yl]carbamate;CS-1037;LGX 818;NSC4820;NSC 4820;NSC-4820;LGX818, >=98%
- CBNumber:
- CB42668617
- Summenformel:
- C22H27ClFN7O4S
- Molgewicht:
- 540.01
- MOL-Datei:
- 1269440-17-6.mol
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Encorafenib (LGX818) Eigenschaften
- Schmelzpunkt:
- 184-185°C
- Dichte
- 1.45±0.1 g/cm3(Predicted)
- storage temp.
- -20°C Freezer, Under inert atmosphere
- L?slichkeit
- DMSO (Slightly), Methanol (Slightly)
- pka
- 5.94±0.10(Predicted)
- Aggregatzustand
- Solid
- Farbe
- White to Off-White
- InChIKey
- CMJCXYNUCSMDBY-ZDUSSCGKSA-N
- SMILES
- C(OC)(=O)N[C@@H](C)CNC1=NC=CC(C2=CN(C(C)C)N=C2C2=CC(Cl)=CC(NS(C)(=O)=O)=C2F)=N1
Sicherheit
- Risiko- und Sicherheitserkl?rung
- Gefahreninformationscode (GHS)
| Bildanzeige (GHS) |
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| Alarmwort |
Warnung
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| Gefahrenhinweise |
| Code |
Gefahrenhinweise |
Gefahrenklasse |
Abteilung |
Alarmwort |
Symbol |
P-Code |
| H302 |
Gesundheitssch?dlich bei Verschlucken. |
Akute Toxizit?t oral |
Kategorie 4 |
Warnung |
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P264, P270, P301+P312, P330, P501 |
| H315 |
Verursacht Hautreizungen. |
Hautreizung |
Kategorie 2 |
Warnung |
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P264, P280, P302+P352, P321,P332+P313, P362 |
| H319 |
Verursacht schwere Augenreizung. |
Schwere Augenreizung |
Kategorie 2 |
Warnung |
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P264, P280, P305+P351+P338,P337+P313P |
| H335 |
Kann die Atemwege reizen. |
Spezifische Zielorgan-Toxizit?t (einmalige Exposition) |
Kategorie 3 (Atemwegsreizung) |
Warnung |
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| 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 M?glichkeit entfernen. Weiter spülen. |
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Encorafenib (LGX818) Chemische Eigenschaften,Einsatz,Produktion Methoden
Beschreibung
Encorafenib (LGX818) is a new-generation BRAF inhibitor that is under evaluation in clinical trials. However, the underlying mechanism remains to be elucidated. Here we show that LGX818 potently decreased ERK phosphorylation and inhibited proliferation in BRAFV600E melanoma cell lines. Moreover, LGX818 downregulated CyclinD1 in a glycogen synthase kinase 3β-independent manner and induced cell cycle arrest in the G1 phase.
Verwenden
LGX 818 is potent and selective BRAFV600E kinase inhibitor and can be used for the treatment of proliferative diseases such as solid tumor diseases.
Trademarks
Braftovi
Biologische Aktivit?t
Encorafenib (LGX818) is a highly potent RAF inhibitor with selective anti-proliferative and apoptotic activity in cells expressing B-RAF(V600E) with EC50 of 4 nM. Phase 3.
Clinical Use
Encorafenib (LGX818) is a new-generation BRAF inhibitor. It is currently under investigation in clinical trials for the treatment of BRAF mutant metastatic melanoma patients . LGX818 induces sustained mitogen-activated protein kinase (MAPK) pathway inhibition and has selective anti-proliferative and apoptotic activity in cells expressing BRAFV600E. However, the mechanism by which LGX818 suppresses BRAF mutant melanoma cell proliferation has not been thoroughly investigated.
Encorafenib (LGX818) Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
Encorafenib (LGX818) Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.
Global( 179)Lieferanten
- LGX 818
- Encorafenib (LGX818)
- Carbamic acid, N-[(1S)-2-[[4-[3-[5-chloro-2-fluoro-3-[(methylsulfonyl)amino]phenyl]-1-(1-methylethyl)-1H-pyrazol-4-yl]-2-pyrimidinyl]amino]-1-methylethyl]-, methyl ester
- LGX 818 (S)-Methyl [1-[[4-[3-[5-chloro-2-fluoro-3-(methylsulfonamido)phenyl]-1-isopropyl-1H-pyrazol-4-yl]pyrimidin-2-yl]amino]propan-2-yl]carbamate
- LGX818, >=98%
- LGX818, Encorafenib
- CS-1037
- methyl N-[(2S)-1-({4-[3-(5-chloro-2-fluoro-3-methanesulfonamidophenyl)-1-(propan-2-yl)-1H-pyrazol-4-yl]pyrimidin-2-yl}amino)propan-2-yl]carbamate
- LGX 818; LGX-818;LGX818
- ENCORAFENIB;LGX818; LGX-818
- LGX818; LGX-818; LGX 818; ENCORAFENIB.
- methyl (S)-(1-((4-(3-(5-chloro-2-fluoro-3-(methylsulfonamido)phenyl)-1-isopropyl-1H-pyrazol-4-yl)pyrimidin-2-yl)amino)propan-2-yl)carbamate
- Encorafenib (LGX818) USP/EP/BP
- Methyl N-[(2s)-1-[[4-[3-[5-chloro-2-fluoro-3-(methanesulfonamido)phenyl]-1-propan-2-ylpyrazol-4-yl]pyrimidin-2-yl]amino]propan-2-yl]carbamate
- NSC 4820
- NSC4820
- NSC-4820
- Cymoxanil Impurity 3
- Encorafenib, 10 mM in DMSO
- (S) - [1 - [[4 - [3 - [5-chloro-2-fluoro-3 - (methylsulfonamido) phenyl] - 1-isopropyl-1h-pyrazole-4-yl] pyrimidin-2-yl] amino] propyl-2-yl] carbamate LGX-818
- (S)-Methyl [1-[[4-[3-[5-chloro-2-fluoro-3-(methylsulfonamido)phenyl]-1-isopropyl-1H-pyrazol-4-yl]pyrimidin-2-yl]amino]propan-2-yl]carbamate
- Encorafenib
- LGX-818
- LGX818
- 1269440-17-6
- C22H27ClFN7O4S
- Inhibitors
