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S1475 AS703026 Is A Novel, Selective, Orally Bioavailable MEK1/2 Inhibitor (Cell IC50 Ranging From 0.005 To 2 M) .
S1475 AS703026 Is A Novel, Selective, Orally Bioavailable MEK1/2 Inhibitor (Cell IC50 Ranging From 0.005 To 2 M) .
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Technical Data:
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M.Wt: 431.20 OH
H +1-713-922-4115
Formula: C15H15FIN3O3 F
O N OH
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H
Solubility: Unknown N
Purity: 99% Tech Support
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Storage: at -20℃ 2 years
(chemistry support)
CAS No.: 1236699-92-5 Synonyms: MSC1936369B techbio@selleckchem.com
(bio support)
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Biological Activity
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AS703026 is a novel, selective, orally bioavailable MEK1/2 inhibitor, in human multiple myeloma
(MM). AS703026 inhibited growth and survival of MM cells (cell IC50 ranging from 0.005 to 2 µM)
and cytokine-induced osteoclast differentiation more potently (9- to 10-fold) 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. Importantly, AS703026 sensitized
MM cells to a broad spectrum of conventional (dexamethasone, melphalan), novel or emerging
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(lenalidomide, perifosine, bortezomib, rapamycin) anti-MM therapies. [1]
References
[1] Kim K et al. Br J Haematol. 2010 May; 149(4):537-49
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