Lifirafenib-BGB-283-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemELifirafenibCat. No.: HY-18957CAS No.: 1446090-77-2Synonyms: BGB-283分式: CHFNO分量: 478.42作靶点: EGFR; Raf作通路: JAK/STAT Signaling; Protein Tyrosine Kinase/RTK;MAPK/ERK Pathway储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-

2、20C 1 month溶解性数据体外实验 DMSO : 125 mg/mL (261.28 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.0902 mL 10.4511 mL 20.9021 mL5 mM 0.4180 mL 2.0902 mL 4.1804 mL10 mM 0.2090 mL 1.0451 mL 2.0902 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。BIOLOGICAL ACTIV

3、ITY物活性 Lifirafenib (BGB-283)新型效的Raf激酶和EGFR抑制剂，对重 组BRafV600E 和EGFR的IC50值分别为23 和29 nM。IC50 & Target EGFR BRafV600E EGFRL858R/T790M1/2 Master of Small Molecules 您边的抑制剂师www.MedChemE29 nM (IC50) 23 nM (IC50) 495 nM (IC50)体外研究 Lifirafenib (BGB-283) potently inhibits BRafV600E-activated ERK phosphorylation

4、 and cell proliferation. Itdemonstrates selective cytotoxicity and preferentially inhibits proliferation of cancer cells harboringBRafV600E and EGFR mutation/amplification. In BRafV600E colorectal cancer cell lines, Lifirafenib (BGB-283) effectively inhibits the reactivation of EGFR and EGFR-mediate

5、d cell proliferation 1.体内研究 Lifirafenib (BGB-283) treatment leads to dose-dependent tumor growth inhibition accompanied by partial andcomplete tumor regressions in both cell line-derived and primary human colorectal tumor xenografts bearingBRafV600E mutation 1.PROTOCOLCell Assay 1 Melanoma, colon, b

6、reast, and lung cancer cells are left to attach for 16 hours and then treated with a 10-pointdilution series in duplicate. CellTiter-Glo reagent is added in each well. Mixture is mixed on an orbital shakerfor 2 minutes to allow cell lysing, followed by 10 minutes incubation at room temperature to al

7、lowdevelopment and stabilization of luminescent signal. Luminescent signal is measured using PHERAstar FSreader. EC50 values for cell viability are determined 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice: When the average tumor size rea

8、ches 110 to 200 mm3, mice are randomized to treatment groups andAdministration 1 treated twice per day or once daily by oral gavage (p.o.) with vehicle alone or 2.5 to 30 mg/kg of BGB-283.As control, mice are treated with erlotinib (100 mg/kg qd) or cetuximab (40 mg/kg twice weekly). Lifirafenib(BGB

9、-283) and erlotinib are formulated at the desired concentration as a homogenous suspension in 0.5%(w/v) methylcellulose in purified water. Cetuximab is formulated by diluting the injection solution with salinebefore dosing 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Tang Z, et al. BGB-283, a Novel RAF Kinase and EGFR Inhibitor, Displays Potent Antitumor Activity in BRAF-Mutated ColorectalCancers. Mol Cancer Ther. 2015 Oct;14(10):2187-97.McePdfHeightCaution: Product has not been fully validated