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Refametinib

Chemical Structure : Refametinib

CAS No.: 923032-37-5

Refametinib (BAY 869766;BAY 86-97661;RDEA-119;RDEA119)

Catalog No.: PC-44028Not For Human Use, Lab Use Only.

Refametinib (BAY 86-97661, RDEA-119) is a potent, non-ATP-competitive, highly selective, allosteric inhibitor of MEK1/2 with IC50 of 19/47 nM respectively.

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Biological Activity

Refametinib (BAY 86-97661, RDEA-119) is a potent, non-ATP-competitive, highly selective, allosteric inhibitor of MEK1/2 with IC50 of 19/47 nM respectively.
Refametinib inhibits anchorage-dependent growth of human cancer cell lines harboring the gain-of-function V600E BRAF mutant with GI50 of 67-89 nM.
Refametinib exhibits complete suppression of ERK phosphorylation at fully efficacious doses in mice and orally bioactive.

Physicochemical Properties

M.Wt 572.3372
Formula C19H20F3IN2O5S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
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Solubility

DMSO: ≥ 31 mg/mL

Chemical Name/SMILES

Cyclopropanesulfonamide, N-[3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]-6-methoxyphenyl]-1-[(2S)-2,3-dihydroxypropyl]-

References

1. Iverson C, et al. Cancer Res. 2009 Sep 1;69(17):6839-47.

2. Chang Q, et al. BMC Cancer. 2010 Sep 28;10:515.

3. Schmieder R, et al. Neoplasia. 2013 Oct;15(10):1161-71.

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