AS-703026 ≥95%
Supplier: ADIPOGEN CORP MS
Synonyms:
(S)-N-(2,3-Dihydroxypropyl)-3-((2-fluoro-4-iodophenyl)amino)isonicotinamide, MSC1936369B, Pimasertib
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 (
Formula:
C₁₅H₁₅FIN₃O₃ MW: 431.2 g/mol Storage Temperature: Refrigerator |
MDL Number:
MFCD16660676 CAS Number: 1236699-92-5 |
Specification Test Results
Purity |
|
Appearance/Color | Solid. |
Solubility |
Soluble in DMSO. Slightly soluble ( |
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