1269440-17-6 Usage
Description
Encorafenib (LGX818) is a new-generation BRAF inhibitor that is under evaluation in clinical trials for its potent and selective inhibition of the BRAFV600E kinase, which plays a crucial role in the development and progression of various proliferative diseases, particularly solid tumor diseases.
Uses
Used in Oncology:
Encorafenib (LGX818) is used as an anticancer agent for the treatment of solid tumor diseases, particularly those driven by the BRAFV600E mutation. It works by potently decreasing ERK phosphorylation and inhibiting proliferation in BRAFV600E melanoma cell lines. Additionally, LGX818 downregulates CyclinD1 in a glycogen synthase kinase 3β-independent manner and induces cell cycle arrest in the G1 phase, thereby exerting inhibitory effects on tumor growth and progression.
Biological Activity
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.
references
[1] stuart d d, li n, poon d j, et al. preclinical profile of lgx818: a potent and selective raf kinase inhibitor. cancer research, 2012, 72(8 supplement): 3790.[2] huang t, karsy m, zhuge j, et al. b-raf and the inhibitors: from bench to bedside. j hematol oncol, 2013, 6(1): 30.
Check Digit Verification of cas no
The CAS Registry Mumber 1269440-17-6 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,2,6,9,4,4 and 0 respectively; the second part has 2 digits, 1 and 7 respectively.
Calculate Digit Verification of CAS Registry Number 1269440-17:
(9*1)+(8*2)+(7*6)+(6*9)+(5*4)+(4*4)+(3*0)+(2*1)+(1*7)=166
166 % 10 = 6
So 1269440-17-6 is a valid CAS Registry Number.
1269440-17-6Relevant articles and documents
COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS
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, (2011/04/14)
The invention provides a novel class of compounds of formula 1, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of B-Raf.
