Molecular Weight(MW): 540.01
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.
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Whole cell lysates from NRAS- or BRAF-mutant melanoma cells treated with encorafenib or/and binimetinib or DMSO as a control for 24 h were subjected to Western blot analysis to detect pERK, ERK and β-Actin. Experiment shown is a representative of three independent experiments.
Clin Cancer Res, 2017, 23(20):6203-6214. Encorafenib (LGX818) purchased from Selleck.
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Choose Selective Raf Inhibitors
|Description||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.|
|Features||Orally bioavailable RAF-selective inhibitor.|
In the A375 (BRAFV600E) human melanoma cell line LGX818 suppresses phospho-ERK (EC50 = 3 nM) leading to potent inhibition of proliferation (EC50 = 4 nM). No significant activity is observed against a panel of 100 kinases (IC50 > 900 nM) and LGX818 does not inhibit proliferation of > 400 cell lines expressing wild-type BRAF. Contributing to the high potency of LGX818 is the extremely slow off-rate from BRAFV600E which is not observed with other RAF inhibitors. In biochemical assays the dissociation half-life is >24 hours which translated into sustained target inhibition in cells following drug wash-out. 
|In vivo||LGX818 treatment at oral doses as low as 6 mg/kg resulted in strong (75%) and sustained (>24 hours) decrease in phospho-MEK, even following clearance of drug from circulation in single dose PK/PD studies in human melanoma xenograft models (BRAFV600E). LGX818 induces tumor regression in multiple BRAF mutant human tumor xenograft models grown in immune compromised mice and rats at doses as low as 1 mg/kg. Consistent with the in vitro data, LGX818 is inactive against BRAF wild-type tumors at doses up to 300 mg/kg bid, with good tolerability and linear increase in exposure. Efficacy is also achieved in a more disease-relevant spontaneous metastatic melanoma and a model of melanoma brain metastasis. LGX818 is a potent and selective RAF kinase inhibitor with unique biochemical properties that contribute to an excellent pharmacological profile. |
|In vitro||DMSO||100 mg/mL (185.18 mM)|
|Ethanol||100 mg/mL (185.18 mM)|
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02109653||Withdrawn||Non-Small Cell Lung Cancer||Array BioPharma||June 2015||Phase 2|
|NCT02263898||Withdrawn||Recurrent Melanoma|Stage IV Melanoma||Jonsson Comprehensive Cancer Center|National Cancer Institute (NCI)||January 2015||Phase 2|
|NCT02278133||Completed||Metastatic Colorectal Cancer||Array BioPharma||December 2014||Phase 1|Phase 2|
|NCT02159066||Active not recruiting||Melanoma||Array BioPharma||July 2014||Phase 2|
|NCT01981187||Completed||Solid Tumor|Hematologic Malignancies||Array BioPharma||January 2014||Phase 2|
|NCT01820364||Terminated||Melanoma||Array BioPharma||November 2013||Phase 2|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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