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Cellagen Technology
MEK1/2 inhibitor
AS-703026 is an orally-available, allosteric inhibitor of MEK1/2 kinases. In multiple myeloma (MM) cell lines, AS-703026 inhibits growth in a dose-dependent manner, with IC50s ranging from 5 nM to 2 uM. Furthermore in INA-6 and U266 cells, AS-703026 exhibited an IC50 of 10 nM and 5 nM, respectively. AS-703026 inhibits proliferation by mediating G0-G1 cell cycle arrest and also induces apoptosis via caspase 3 and PARP cleavage in MM cells. (1)
AS-703026 specifically inhibits MEK's downstream target kinase ERK on the average of 5-fold more potently than AZD6244. Additionally, cetuximab-resistant colorectal cancer cell lines were inhibited by AS-703026, displaying its efficacy against K-ras mutations. (2)
Cellagen Technology
MEK1/2 inhibitor
AS-703026 is an orally-available, allosteric inhibitor of MEK1/2 kinases. In multiple myeloma (MM) cell lines, AS-703026 inhibits growth in a dose-dependent manner, with IC50s ranging from 5 nM to 2 uM. Furthermore in INA-6 and U266 cells, AS-703026 exhibited an IC50 of 10 nM and 5 nM, respectively. AS-703026 inhibits proliferation by mediating G0-G1 cell cycle arrest and also induces apoptosis via caspase 3 and PARP cleavage in MM cells. (1)
AS-703026 specifically inhibits MEK's downstream target kinase ERK on the average of 5-fold more potently than AZD6244. Additionally, cetuximab-resistant colorectal cancer cell lines were inhibited by AS-703026, displaying its efficacy against K-ras mutations. (2)
