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Refametinib

Catalog No.
B1267
MEK 1/ MEK 2 inhibitor
Grouped product items
SizePriceStock Qty
5mg
$70.00
In stock
10mg
$105.00
In stock
50mg
$290.00
In stock
100mg
$470.00
In stock
200mg
$760.00
In stock

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Email: [email protected]

Worldwide Distributors

Background

Refametinib is a selective and orally available allosteric inhibitor of MEK 1 and MEK 2 with IC50 values of 19nM and 47nM, respectively [1].

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].

References:
[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.

Product Citation

Chemical Properties

StorageStore at -20°C
M.Wt572.34
Cas No.923032-37-5
FormulaC19H20F3IN2O5S
Solubility≥151.8mg/mL in DMSO
Chemical NameN-[3,4-difluoro-2-(2-fluoro-4-iodoanilino)-6-methoxyphenyl]-1-[(2S)-2,3-dihydroxypropyl]cyclopropane-1-sulfonamide
SDFDownload SDF
Canonical SMILESCOC1=CC(=C(C(=C1NS(=O)(=O)C2(CC2)CC(CO)O)NC3=C(C=C(C=C3)I)F)F)F
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Biological Activity

Description Refametinib (RDEA119, Bay 86-9766) is a potent, ATP non-competitive and highly selective inhibitor of MEK1 and MEK2 with IC50 values of 19 nM and 47 nM, respectively.
Targets MEK1 MEK2        
IC50 19 nM 47 nM        

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