2274819-46-2

LUT014 is a topical inhibitor targeting BRAF that cannot pass through the blood-brain barrier. LUT014 inhibits BRAF kinase and abnormally activates the MAPK/ERK signaling pathway, promoting the proliferation of epidermal keratinocytes, repairing skin barrier damage caused by radiation damage, and alleviating inflammatory responses. LUT014 is independent of RAS signaling and accelerates the repair and regeneration of damaged skin cells. LUT014 can be used to study radiation dermatitis, especially skin damage caused by breast cancer radiotherapy[1][2][3].

B-Raf: 11.7 nM (IC₅₀)

[1] Katz S, et al. A topical BRAF inhibitor (LUT-014) for treatment of radiodermatitis among women with breast cancer. JAAD Int. 2023 Dec 25;15:62-68. DOI:10.1016/j.jdin.2023.11.009
[2] Wang PP, et al. BRAF Mutations in Colorectal Liver Metastases: Prognostic Implications and Potential Therapeutic Strategies. Cancers (Basel). 2022 Aug 23;14(17):4067. DOI:10.3390/cancers14174067
[3] Li Y, et al. Mechanism of Lethal Skin Toxicities Induced by Epidermal Growth Factor Receptor Inhibitors and Related Treatment Strategies. Front Oncol. 2022 Feb 10;12:804212. DOI:10.3389/fonc.2022.804212