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Discovery Miles 6 750
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Selumetinib (AZD6244, ARRY-142886), activating mutations in the
BRAF gene, primarily at V600E, are associated with poorer outcomes
in patients with papillary thyroid cancer. MAPK kinase (MEK),
immediately downstream of BRAF, is a promising target for MAPK/ERK
pathway inhibition. In addition to thyroid cancer, BRAF-activating
mutations are prevalent in melanoma (-59%), colorectal cancer
(5-22%), serous ovarian cancer (-30%), and several other tumor
types. Four lines bearing V600E BRAF mutations were all sensitive
to selumetinib, with GI50 clarification needed] values ranging from
14 to 50 nM. A positive control BRAF mutant melanoma line, SKMel28,
exhibited a similar GI50 of 23 nM. A Phase II clinical trial about
selumetinib in cancers with BRAF mutations is ongoing.
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