e6201

E6201 is a synthetic small-molecule, ATP-competitive dual kinase inhibitor that targets mitogen-activated protein kinase kinase 1 (MEK1) and fms-like tyrosine kinase 3 (FLT3). It inhibits MEK1-induced ERK2 phosphorylation, MKK4-induced JNK phosphorylation, and MKK6-induced p38 MAPK phosphorylation. E6201 has demonstrated anti-tumor efficacy in preclinical models of various cancers, including triple-negative breast cancer and BRAF V600E-mutant metastatic melanoma with brain metastases. It also exhibits anti-inflammatory activity by inhibiting proinflammatory cytokine production and hyperproliferation of keratinocytes, suggesting potential utility in inflammatory diseases such as psoriasis. The drug has been investigated in clinical trials for chronic plaque psoriasis (discontinued), acute myeloid leukemia, chronic myelomonocytic leukemia, myelodysplastic syndromes (Phase I/II), and brain metastases (Phase I). E6201 was originally developed by Eisai[2][3][4][5].

Other names

UNII-CZP9GB25HOUNII-CZP-9GB25HOUNII-CZP 9GB25HO603987-35-5