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Encorafenib

Chemical Structure : Encorafenib

CAS No.: 1269440-17-6

Encorafenib (NVP-LGX818, LGX818, LGX-818)

Catalog No.: PC-49770Not For Human Use, Lab Use Only.

Encorafenib (NVP-LGX818, LGX818) a potent, selective BRAF inhibitor with IC50 of 0.35, 0.47, and 0.3 nM against BRAF V600E, wild-type BRAF and CRAF in vitro cell-free assays, respectively.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Encorafenib (NVP-LGX818, LGX818) a potent, selective BRAF inhibitor with IC50 of 0.35, 0.47, and 0.3 nM against BRAF V600E, wild-type BRAF and CRAF in vitro cell-free assays, respectively.
Encorafenib (NVP-LGX818, LGX818) is able to bind to other kinases in vitro including JNK1, JNK2, JNK3, LIMK1, LIMK2, MEK4, and STK36 and significantly reduce ligand binding to these kinases at clinically achievable concentrations (<0.9 uM).
Encorafenib (NVP-LGX818, LGX818) inhibited the in vitro cell growth of tumor cell lines that express BRAF V600 E, D, and K mutations.
Encorafenib (NVP-LGX818, LGX818) induced tumor regressions associated with RAF/MEK/ERK pathway suppression in mice implanted with tumor cells expressing the BRAF V600E mutation.

Physicochemical Properties

M.Wt 540.01
Formula C22H27ClFN7O4S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

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

References

1. Adelmann CH, et al. Oncotarget. 2016 May 24;7(21):30453-60.

2. Krepler C, et al. Clin Cancer Res. 2016 Apr 1;22(7):1592-602.

3. van Geel RMJM, et al. Cancer Discov. 2017 Jun;7(6):610-619.

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