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Submit ReviewLY 3009120 is a potent pan-Raf kinase inhibitor (IC50 values are 31 - 47, 42 and 44 nM for b-RAF, c-RAF and a-RAF in A375 cells, respectively). Also inhibits kinase activity of Raf hetero- and homodimers. Displays antiproliferative effects against b-RAF and Ras mutant melanoma cells. Inhibits MEK and ERK phosphorylation, and b-RAF and Ras mutant tumor growth in mouse xenograft models.
分子量 | 424.52 |
公式 | C23H29FN6O |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 1454682-72-4 |
PubChem ID | 71721540 |
InChI Key | HHCBMISMPSAZBF-UHFFFAOYSA-N |
Smiles | CNC1=NC2=C(C=N1)C=C(C(C)=N2)C1=CC(NC(=O)NCCC(C)(C)C)=C(F)C=C1C |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
参考文献是支持产品生物活性的出版物。
Henry et al (2015) Discovery of 1-(3,3-dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)urea (LY3009120) as a pan-RAF inhibitor with minimal paradoxical activation and activity against BRAF or RAS mutant tumor cells. J.Med.Chem. 58 4165 PMID: 25965804
Peng et al (2015) Inhibition of RAF isoforms and active dimers by LY3009120 leads to anti-tumor activities in RAS or BRAF mutant cancers. Cancer Cell. 28 384 PMID: 26343583
关键词: LY 3009120, LY 3009120 supplier, LY3009120, potent, pan, raf, inhibitors, inhibition, bRAf, cRAF, aRAF, inhibits, Raf, Kinase, 6854, Tocris Bioscience
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