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Refametinib (RDEA-119, BAY 86-9766)

MEK1/2 inhibitor

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Catalog No. A12866

Availability:Stock in USAIn stock

Product Name Catalog No. Price Qty
Refametinib (RDEA-119, BAY 86-9766) 10mg A12866-10
Refametinib (RDEA-119, BAY 86-9766) 25mg A12866-25
Refametinib (RDEA-119, BAY 86-9766) 50mg A12866-50
Refametinib (RDEA-119, BAY 86-9766) 100mg A12866-100

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Quick Overview

Refametinib, also known as RDEA119, BAY 86-9766, is an orally bioavailable selective MEK inhibitor with potential antineoplastic activity.

Refametinib (RDEA-119, BAY 86-9766)

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Chemical Information

Catalog Num A12866
Actions Inhibitor
M. Wt 572.34
Formula C19H20F3IN2O5S
Solubility DMSO
Purity >98%
Storage at -20°C 3 years Powder
CAS No. 923032-38-6
Synonyms RDEA119, RDEA 119, BAY 86-9766, BAY 869766, BAY869766
SMILES COC1=CC(=C(C(=C1NS(=O)(=O)C2(CC2)C[[email protected]](CO)O)NC3=C(C=C(C=C3)I)F)F)F

Biological Activity

Refametinib, also known as RDEA119, BAY 86-9766, is an orally bioavailable selective MEK inhibitor with potential antineoplastic activity.

Preparing Stock Solutions

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.1 mM 17.47 mL 87.36 mL 174.72mL
0.5 mM 3.49 mL 17.47 mL 34.94 mL
1 mM 1.75 mL 8.74 mL 17.47 mL
5 mM 0.35 mL 1.75 mL 3.49 mL

*The above data is based on the productmolecular weight 572.34. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Refametinib is a non–ATP-competitive inhibitor of MEK1/2. It inhibits MEK activity in an in vitro assay with IC50 values of 19nM and 47nM for MEK1 and MEK2, respectively. X-ray shows refametinib binds to an allosteric site of MEK. It does not affect ATP binding but precludes binding to the substrate ERK, thus preventing ERK phosphorylation. Refametinib inhibits MEK with EC50 values ranging from 2.5nM to 15.8nM in a variety of human cancer cells including A375, Colo205, HT-29 and MDA-MB-231. In addition, in the cancer cell lines harboring V600E BRAF mutant, refametinib suppresses cell growth with GI50 values ranging from 67nM to 89nM. Furthermore, in the human melanoma A375 tumor xenograft model, treatment of refametinib causes obvious tumor growth delay and regression. Refametinib also shows tumor growth inhibition in the xenograft model of human Colo205 tumor [1].

[1] Iverson C, Larson G, Lai C, et al. RDEA119/BAY 869766: a potent, selective, allosteric inhibitor of MEK1/2 for the treatment of cancer. Cancer research, 2009, 69(17): 6839-6847.

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