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首页-小分子抑制剂&激动剂-Ras-Raf-MAPK-ERK Pathway-Raf-Encorafenib
Encorafenib

Chemical Structure : Encorafenib

CAS No.: 1269440-17-6

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

货号: 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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10 mg ￥1180 In stock
25 mg ￥2180 In stock
50 mg ￥3580 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 540.01
分子式 C22H27ClFN7O4S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
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

参考文献

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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