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AS-703026 (Pimasertib) | MEK1/2 inhibitor

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Price:
$89.00
Catalog #:
C2770-5
Quantity:


Product Description

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)


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

Other Information:

Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.

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