| Identification | Back Directory | [Name]
Urea, N-[2-fluoro-4-methyl-5-[2-methyl-7-(methylamino)-1,6-naphthyridin-3-yl]phenyl]-N′-[(2S)-2-hydroxy-3,3-dimethylbutyl]- | [CAS]
1455031-68-1 | [Synonyms]
Urea, N-[2-fluoro-4-methyl-5-[2-methyl-7-(methylamino)-1,6-naphthyridin-3-yl]phenyl]-N′-[(2S)-2-hydroxy-3,3-dimethylbutyl]- | [Molecular Formula]
C24H30FN5O2 | [MOL File]
1455031-68-1.mol | [Molecular Weight]
439.53 |
| Chemical Properties | Back Directory | [Boiling point ]
573.6±50.0 °C(predicted) | [density ]
1.242±0.06 g/cm3(Temp: 20 °C; Press: 760 Torr)(predicted) | [pka]
13.26±0.46(predicted) |
| Hazard Information | Back Directory | [Uses]
LSN3074753, an analog of LY3009120 (HY-12558), is a pan-RAF and Raf dimer inhibitor. LSN3074753 demonstrates activity against tumor cells with MAPK pathway activation driven by BRAF monomer or RAF dimers including BRAF- or KRAS-mutant colorectal cancer. LSN3074753 combined with Cetuximab (HY-P9905) shows additive and synergistic effects for colorectal cancer PDX models, particularly those with KRAS or BRAF mutation[1][2]. | [References]
[1] Yao YM, et al. Mouse PDX Trial Suggests Synergy of Concurrent Inhibition of RAF and EGFR in Colorectal Cancer with BRAF or KRAS Mutations. Clin Cancer Res. 2017 Sep 15;23(18):5547-5560. DOI:10.1158/1078-0432.CCR-16-3250
[2] Sorokin A, et al. Antitumor activity of panRAF inhibition in BRAF V600E metastatic colorectal cancer[J]. 2017. |
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