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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||
DMSO ≥83mg/mL Water <1.2mg/mL Ethanol ≥2.6mg/mL
|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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BIX02188 is a selective inhibitor of MEK5 with IC50 of 4.3 nM, also inhibits ERK5 catalytic activity with IC50 of 810 nM, and does not inhibit closely related kinases MEK1, MEK2, ERK2, and JNK2.
BIX02189 is a selective MEK5/ERK5 inhibitor with an IC50 of 59 nM.
GDC-0623 is a potent, ATP-uncompetitive inhibitors of MEK1(Ki=0.13 nM, (addition)ATP); 6-fold weaker potency against HCT116 (KRAS(G13D), EC50=42 nM) versus A375 (BRAF(V600E), EC50=7 nM).
MEK inhibitor is a potent MEK inhibitor, antitumor agent.
MEK162(ARRY-438162; ARRY-162) is a potent inhibitor of MEK1/2 with IC50 of 12 nM.
OTS964 is a potent TOPK inhibitor with an IC50 value of 28 nM.
PD318088 is a non-ATP competitive allosteric MEK1/2 inhibitor, binds simultaneously with ATP in a region of the MEK1 active site that is adjacent to the ATP-binding site.