Discovery of a novel pan-RAF inhibitor with potent anti-tumor activity in preclinical models of BRAFV600E mutant cancer.

doi:10.1016/j.lfs.2017.06.021

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Article

Discovery of a novel pan-RAF inhibitor with potent anti-tumor activity in preclinical models of BRAFV600E mutant cancer.

Life sciences - 15 Aug 2017

Hong Sung Pyo, Ahn Soon Kil

Abstract excerpt

AIMS: BRAF mutations, especially BRAF V600E, are a frequent occurrence in malignant melanomas. The BRAF inhibitors are used as the care standard for BRAF-mutant metastatic melanomas. However, melanomas rapidly develop resistance to BRAF inhibitors after a median response duration of 6months, and the subsequent rapid development of cutaneous toxicity is enhanced by the paradoxical activation of CRAF. In this...

Topics

Animals
Antineoplastic Agents
Cell Line, Tumor
Colorectal Neoplasms
Female
Humans
MAP Kinase Signaling System
Male
Melanoma
Mice
Mice, Inbred BALB C
Mice, Inbred ICR
Mice, Nude
Mutation
Protein Kinase Inhibitors
Proto-Oncogene Proteins B-raf
Purines
Rats

Source

Open in PubMed

Identifiers

PMID: 28645859
DOI: 10.1016/j.lfs.2017.06.021

Genes

BRAF

Variants

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 30 Aug 2026.

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