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Home   »   Product Pathways  »  MEK  »  AS703026

Products are for research use only. Not for human use. We do not sell to patients.

CS-0198 AS703026

(Pimasertib;MSC1936369B;AS-703026;AS 703026)
Structure Price and Availability of    AS703026
United States
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5mg $50 In-stock Inquiry
10mg $65 In-stock
50mg $180 In-stock
100mg $287 In-stock
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 Distributor In Japan:  フナコシ株式会社    電話番号:81-3-5684-1620   
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AS703026  M.Wt:  431.2
AS703026  Formula: C15H15FIN3O3
AS703026  Solubility: DMSO ≥83mg/mL Water <1.2mg/mL Ethanol ≥2.6mg/mL
AS703026  Purity: >98%
AS703026  Storage:  Please store the product under the recommended conditions in the Certificate of Analysis.
CAS: 1236699-92-5

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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. IC50 value: Target: MEK1/2 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). [1] 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). [2] 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. [1] 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. [2]

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