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Products are for research use only. Not for human use. We do not sell to patients.
(Pimasertib; MSC1936369B; AS-703026; AS 703026)
AS703026 Chemical Structure
|Product name: AS703026|
|Cat. No.: HY-12042|
AS703026(Pimasertib) is a highly selective, potent, ATP non-competitive allosteric inhibitor of MEK1/2 with IC50 of 5 nM-2 μM in MM cell lines.
in vitro: AS703026 is a novel, selective, orally bioavailable MEK1/2 inhibitor that binds to the distinctive MEK allosteric site and therefore exhibits exquisite kinase selectivity. AS703026 inhibits growth and survival of human multiple myeloma (MM) cells, including U266 and INA-6, with IC50 of 5 nM and 11 nM, respectively. Such an inhibitory effect by AS703026 is mediated by G0-G1 cell cycle arrest and is accompanied by reduced expresson of the MAF oncogene. AS703026 further induces apoptosis via caspase-3 and PARP cleavage in MM cells, both in the presence or absence of bone marrow stromal cells (BMSCs).  AS703026 may be an effective therapy in colorectal cancer caused by K-Ras mutation. AS703026 (10 μM) effectively inhibits the ERK pathway, proliferation, and transformation in human DLD-1 colorectal cancer cells what carry a mutant allele of K-Ras (D-MUT). 
in vivo: AS703026 (15 and 30 mg/kg) significantly inhibits tumor growth in a human plasmacytoma xenograft model of H929 MM cells. This can be correlated with downregulated pERK1/2, induced PARP cleavage, and decreased microvessels.  AS703026 (10 mg/kg) inhibits tumor growth, and markedly decreases p-ERK level in a xenograft mouse model of human K-Ras mutated (D-MUT) colorectal tumor. 
|M.Wt||431.2||Storage||Please store the product under the recommended conditions in the Certificate of Analysis.|
|Solvent & Solubility||
10 mM in DMSO
|1 mg||5 mg||10 mg|
|1 mM||2.3191 mL||11.5955 mL||23.1911 mL|
|5 mM||0.4638 mL||2.3191 mL||4.6382 mL|
|10 mM||0.2319 mL||1.1596 mL||2.3191 mL|
|Product Name||Sponsor Only||Condition||Start Date||End Date||Phase||Last Change Date|
|AS703026||EMD Serono Inc||Peritoneal tumor||30-SEP-13||31-MAR-16||Phase 2||13-SEP-13|
|EMD Serono Inc||Ovary tumor||30-SEP-13||31-MAR-16||Phase 2||13-SEP-13|
|EMD Serono Inc||Pancreas tumor||30-NOV-09||31-AUG-15||Phase 2||20-JUN-13|
|EMD Serono Inc||Melanoma||30-NOV-12||31-OCT-14||Phase 2||27-MAR-13|
|EMD Serono Inc||Adenocarcinoma||30-NOV-09||31-AUG-15||Phase 2||20-JUN-13|
|EMD Serono Inc||Metastatic colorectal cancer||31-MAR-10||31-MAY-13||Phase 2||23-OCT-13|
. Kim K, et al. Blockade of the MEK/ERK signalling cascade by AS703026, a novel selective MEK1/2 inhibitor, induces pleiotropic anti-myeloma activity in vitro and in vivo. Br J Haematol, 2010, 149(4), 537-549.
. Yoon J, et al. MEK1/2 inhibitors AS703026 and AZD6244 may be potential therapies for KRAS mutated colorectal cancer that is resistant to EGFR monoclonal antibody therapy. Cancer Res, 2011, 71(2), 445-453
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