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Association details:
| Biomarker: | MAP2K1 C121S |
|---|---|
| Cancer: | Melanoma |
| Drug: | E6201 (FLT3 inhibitor, MEK1 inhibitor, MEK2 inhibitor, ACVR1 inhibitor, MAP3K1 inhibitor) |
| Direction: | Sensitive |
Evidence:
Source:
Title:
Novel ATP-competitive MEK inhibitor E6201 is effective against vemurafenib-resistant melanoma harboring the MEK1-C121S mutation in a preclinical model
Excerpt:
We found that the acquired MEK1-C121S mutation in BRAF-V600E mutant melanoma conferred resistance to both vemurafenib and selumetinib but not E6201. The effectiveness of E6201 in this preclinical study is a result of its binding with MEK1 far from the C121S point mutation so the mutation is unable to influence the MAPK pathway inhibitory activity. These results support further clinical investigation of E6201.
DOI:
10.1158/1535-7163.MCT-13-0667
