AVANTI POLAR LIPIDS , CYGNUS , LARODAN , ADIPOGEN , MYBIOSOURCE , SERVA NORDMARK, BIOWORLD, EDGEBIO , PANREAC APPLICHEM
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Product description: AS703026 is a novel, selective, non-competitive, orally bioavailable MEK1/2 inhibitor with experimental IC(50) values of 5-11nM. In use on multiple myeloma cells (MM), AS703026 inhibited growth and survival of MM cells and cytokine-induced osteoclast differentiation more potently (~10X) than AZD6244. Inhibition of proliferation induced by AS703026 was mediated by G0-G1 cell cycle arrest and was accompanied by reduction of MAF oncogene expression. AS703026 further induced apoptosis via caspase 3 and Poly ADP ribose polymerase (PARP) cleavage in MM cells, both in the presence or absence of bone marrow stromal cells (BMSCs). Importantly, AS703026 sensitized MM cells to a broad spectrum of conventional (dexamethasone, melphalan), novel or emerging (lenalidomide, perifosine, bortezomib, rapamycin) anti-MM therapies. Significant tumour growth reduction in AS703026- vs. vehicle-treated mice bearing H929 MM xenograft tumours correlated with downregulated pERK1/2, induced PARP cleavage, and decreased microvessels in vivo. Moreover, AS703026 (<200nM) was cytotoxic against the majority of tumour cells tested from patients with relapsed and refractory MM (84%), regardless of mutational status of RAS and BRAF genes. Importantly, BMSC-induced viability of MM patient cells was similarly blocked within the same dose range.
Alternate Names/Synonyms: AS703026
Product Type: Chemical
Molecular Formula: C15H15FIN3O3
Molecular Weight: 431.2
Solubility: Soluble in DMSO. Slightly soluble (<1mg/ml) in ethanol.
Short Term Storage: +4°C
Long Term Storage: +4°C
Use & Stability: Stable for at least 1 year after receipt when stored at +4°C.
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