Encorafenib

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

LGX818是一种口服的突变BRaf V600E抑制剂(IC50=0.3 nM)，具有潜在的抗肿瘤活性。

Encorafenib, also known as LGX-818, is an orally available Raf kinase inhibitor with potential antineoplastic activity. LGX818 specifically inhibits Raf kinase, a serine/threonine enzyme in the RAF/mitogen-activated protein kinase kinase (MEK)/extracellular signal-related kinase (ERK) signaling pathway. By inhibiting the activation of the RAF/MEK/ERK signaling pathway, the administration of LGX818 may result in a decrease in proliferation of tumor cells.(In Vitro):Encorafenib (LGX818) is a potent drug that can prevents diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of B-Raf. Encorafenib (LGX818) (10 nM) suppresses the ERK/MAPK pathway and displays marked inhibition of pERK in A375, G361 and SK-MEL-24 cells. 10 nM Encorafenib (LGX818) treatment for 12 days potently inhibits colony formation in A375, G361 and SK-MEL-24 cells, but not in RPMI7951 and C8161 cells. Encorafenib (LGX818) treatment induces a steady increase in the β-catenin level in G361 cells over time.

Encorafenib (LGX818) is a potent drug that can prevents diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of B-Raf. Encorafenib (LGX818) (10 nM) suppresses the ERK/MAPK pathway and displays marked inhibition of pERK in A375, G361 and SK-MEL-24 cells. 10 nM Encorafenib (LGX818) treatment for 12 days potently inhibits colony formation in A375, G361 and SK-MEL-24 cells, but not in RPMI7951 and C8161 cells. Encorafenib (LGX818) treatment induces a steady increase in the β-catenin level in G361 cells over time.

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LGX818 | LGX-818 | LGX 818 | Encorafenib

Cell Cycle/DNA Damage

HDAC

B-Raf (V600E)

Cancer

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1269440-17-6

540.01

C22H27ClFN7O4S

>98% (HPLC)

DMSO : 50 mg/mL 92.59 mM;

C[C@@H](CNC1=NC=CC(=N1)C2=CN(N=C2C3=CC(=CC(=C3F)NS(=O)(=O)C)Cl)C(C)C)NC(=O)OC

(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.

(-20℃)

With Ice Pack

≥ 2 years