AS703026
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CAS No. | 1236699-92-5 | Cat. No. | BCP02094 |
Name | AS703026 | ||
Synonyms | AS 703026;AS-703026;Pimasertib; | ||
SMILES | |||
Chemical Name | |||
Formula | C15H15FIN3O3 | M. Wt | 431.2 |
Purity | 98% | Storage | Store at 4-8°C |
Description | 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). |
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