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Apexbio Technology LLC Refametinib 923032-37-5 200mg

Supplier: Apexbio Technology LLC B1267200
Refametinib (CAS 923032-37-5) is an orally bioavailable selective allosteric inhibitor of mitogen-activated protein kinase kinases MEK1 and MEK2 It binds to an allosteric site distinct from the ATP-binding pocket thereby inhibiting MEK1 and MEK2 enzymatic activity (IC50 19 nM and 47 nM respectively) and blocking phosphorylation of ERK without interfering with ATP binding Refametinib demonstrates potent inhibition in human tumor cell lines with EC50 values ranging from 2 5 to 15 8 nM and suppresses proliferation in BRAF V600E-mutant lines (GI50 67 89 nM) It induces tumor growth delay and regression in xenograft models supporting its utility in cancer research
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