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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 MEKs 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)
Technical information:
| Chemical Formula: | C15H15FIN3O3 | |
| CAS #: | 1236699-92-5 | |
| Molecular Weight: | 431.2 | |
| Purity: | > 99% | |
| Appearance: | White | |
| Chemical Name: | (S)-N-(2,3-dihydroxypropyl)-3-(2-fluoro-4-iodophenylamino)isonicotinamide - See more at: http://www.selleckchem.com/products/AS703026.html#sthash.ajQXgXLc.dpuf | |
| Solubility: | Up to 100 mM in DMSO | |
| Synonyms: | AS-703026, AS703026, Pimasertib, MSC1936369B |
Shipping Condition: The product is shipped in a glass vial at ambient temperature. Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
| 1. | Kim et al., Blockade of the MEK/ERK signalling cascade by AS703026, a novel selective MEK1/2 inhibitor, induces peliotropic anti-myeloma activity in vitro and in vivo. Br. J. Haematol. 2010, 149, 537-549. Pubmed ID: 20331454 |
| 2. | Yoon 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, 445-453. Pubmed ID: 21118963 |