产品说明书

Lifirafenib

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Chemical Structure| 1446090-79-4 同义名 : BGB-283;Beigene-283
CAS号 : 1446090-79-4
货号 : A266866
分子式 : C25H17F3N4O3
纯度 : 96%
分子量 : 478.423
MDL号 : MFCD30489379
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(219.47 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • EGFR/ErbB1

    EGFR, IC50:29 nM

  • mutant EGFR

    EGFR(T790M/L858R), IC50:495 nM

  • B-Raf

    BRAF(V600E), IC50:23 nM

    BRAF WT, IC50:32 nM

  • C-Raf/Raf-1

    C-RAF (Y340/341D), IC50:7 nM

  • A-raf

    WT A-RAF, IC50:1 nM
描述 Lifirafenib (BGB-283) is a potent inhibition of BRafV600E-activated ERK phosphorylation and cell proliferation, displaying selective cytotoxicity towards cancer cells with BRafV600E mutations and EGFR mutations/amplifications. It notably impedes the reactivation of EGFR and EGFR-mediated cell proliferation in BRafV600E colorectal cancer cell lines[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.09mL

0.42mL

0.21mL

10.45mL

2.09mL

1.05mL

20.90mL

4.18mL

2.09mL
参考文献

[1]Tang Z, et al. BGB-283, a Novel RAF Kinase and EGFR Inhibitor, Displays Potent Antitumor Activity in BRAF-Mutated Colorectal Cancers. Mol Cancer Ther. 2015 Oct;14(10):2187-97.