What is the Encorafenib (LGX818)?

Encorafenib (LGX818) is , while it's Molecular Formula is C22H27ClFN7O4S. LGX 818 is potent and selective BRAFV600E kinase inhibitor and can be used for the treatment of proliferative diseases such as solid tumor diseases.

What is the CAS number for Encorafenib (LGX818)?

The CAS number of Encorafenib (LGX818) is 1269440-17-6.

What is Encorafenib (LGX818) (1269440-17-6) used for?

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.

What is the Encorafenib (LGX818)?

Encorafenib (LGX818) is , while it's Molecular Formula is C22H27ClFN7O4S. LGX 818 is potent and selective BRAFV600E kinase inhibitor and can be used for the treatment of proliferative diseases such as solid tumor diseases.

What is the CAS number for Encorafenib (LGX818)?

The CAS number of Encorafenib (LGX818) is 1269440-17-6.

What is Encorafenib (LGX818) (1269440-17-6) used for?

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.

Product Class

1269440-17-6

Product Name：Encorafenib
Molecular Formula：C22H27ClFN7O4S
Purity：99%
Molecular Weight：540.018

Inquiry

Product Details:

CasNo： 1269440-17-6

Molecular Formula： C22H27ClFN7O4S

Quality Manufacturer Supply Top Purity 99% Encorafenib 1269440-17-6 Competitive Price

Molecular Formula:C22H27ClFN7O4S
Molecular Weight:540.018
PKA:5.94±0.10(Predicted)
PSA：152.00000
Density:1.45±0.1 g/cm3(Predicted)
LogP:5.33960

Encorafenib(Cas 1269440-17-6) Usage

Overview	Encorafenib is a medication sold under the brand name Braftovi, and it is used in the treatment of certain melanoma cancers. It belongs to the class of medications called kinase inhibitors and specifically acts as a small molecule BRAF inhibitor.
Chemical Structure	Encorafenib is a small molecule drug, but its detailed chemical structure is not provided in the information. The term "small molecule" indicates that it is a low molecular weight compound.
Mechanism of Action	Encorafenib functions as a BRAF inhibitor, targeting key enzymes in the MAPK (Mitogen-Activated Protein Kinase) signaling pathway. This pathway plays a crucial role in the regulation of cell growth and division. Aberrations in this pathway are often observed in various cancers, including melanoma and colorectal cancers.
Indications	Encorafenib is primarily used for the treatment of certain types of melanoma cancers. It is designed to inhibit the growth and division of melanoma cells by interfering with the signals within cancer cells that promote their continuous growth.
Combination Therapy	Encorafenib is sometimes used in combination with another chemotherapy drug called binimetinib (enco-bini). This combination is aimed not only at killing melanoma cells but also at preventing the development of new skin cancers.

1269440-17-6 Relevant articles

COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS

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Page/Page column 58-59, (2011/04/14)

The invention provides a novel class of ...

Phase I Dose-Escalation and -Expansion Study of the BRAF Inhibitor Encorafenib (LGX818) in Metastatic BRAF-Mutant Melanoma

Jean-Pierre Delord; Caroline Robert; Marta Nyakas; Grant A. McArthur; Ragini Kudchakar; Amit Mahipal; Yasuhide Yamada; Ryan Sullivan; Ana Arance; Richard F. Kefford; Matteo S. Carlino; Manuel Hidalgo; Carlos Gomez-Roca; Daniela Michel; Abdelkader Seroutou; Vassilios Aslanis; Giordano Caponigro; Darrin D. Stuart; Laure Moutouh-de Parseval; Tim Demuth; Reinhard Dummer

CANCER THERAPY: CLINICAL, Volume 23, Issue 18 15 September 2017

Encorafenib monotherapy was then tested across a range of once-daily (50–700 mg) or twice-daily (75–150 mg) regimens in a phase I, open-label, dose-escalation and -expansion study in adult patients with histologically confirmed advanced/metastatic BRAF-mutant melanoma. Study objectives were to determine the maximum tolerated dose (MTD) and/or recommended phase II dose (RP2D), characterize the safety and tolerability and pharmacokinetic profile, and assess the preliminary antitumor activity of encorafenib.

1269440-17-6 Process route

: 1269440-99-4
(S)-methyl 1-(4-(3-(5-chloro-2-fluoro-3-(N-(methylsulfonyl)methylsulfonamido)phenyl)-1-isopropyl-1H-pyrazol-4-yl)pyrimidin-2-ylamino)propan-2-ylcarbamate

: 1269440-17-6
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

Conditions

Conditions	Yield
(S)-methyl 1-(4-(3-(5-chloro-2-fluoro-3-(N-(methylsulfonyl)methylsulfonamido)phenyl)-1-isopropyl-1H-pyrazol-4-yl)pyrimidin-2-ylamino)propan-2-ylcarbamate; With sodium hydroxide; In 2-methyltetrahydrofuran; water; at 20 - 23 ℃; for 0.5h; With hydrogenchloride; In 2-methyltetrahydrofuran; water; pH=6 - 6.5; With sodium hydrogencarbonate; In 2-methyltetrahydrofuran; water; pH=8.5;

: 1269440-76-7
(S)-methyl 1-(4-(3-(3-amino-2-chloro-5-fluorophenyl)-1-isopropyl-1H-pyrazol-4-yl)pyrimidin-2-ylamino)propan-2-ylcarbamate

: 124-63-0
methanesulfonyl chloride

: 1269440-17-6
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