1455031-68-1
Chemical Structure
LSN3074753
- CAS No.: 1455031-68-1
- Formula:C24H30FN5O2
- Molecular Weight:439.53
InChIKey: YBTZROQGXQXJCA-OAQYLSRUSA-N
SMILES: O=C(NC[C@@H](O)C(C)(C)C)NC1=CC(C2=CC3=CN=C(NC)C=C3N=C2C)=C(C)C=C1F
Biological Activity: 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].
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LSN3074753 | 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. | |||||||||||||||||||||
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- [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. [Content Brief]
- [2]. Sorokin A, et al. Antitumor activity of panRAF inhibition in BRAF V600E metastatic colorectal cancer[J]. 2017.
Keywords
