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Product Details

Binimetinib | MEK1/2 inhibitor

Binimetinib (606143-89-9) is a potent (IC50 = 12 nM) and selective allosteric inhibitor of MEK1/2.1,2 Recently approved by the FDA for treatment of melanoma in combination with Encorafenib. Binimetinib has had limited success as monotherapy but has shown promise in combination with other chemotherapeutic agents.3-5

References/Citations

1) Lee et al. (2010), Preclinical development of ARRY-162, a potent and selective MEK1/2 inhibitor; Cancer Res. 70 2515
2) Winski et al. (2010), MEK162 (ARRY-162), a novel MEK ½ inhibitor, inhibits tumor growth regardless of KRAS/RAF pathway mutations; EJC Supplements 56
3) Lee et al. (2016), Efficacy of the combination of MEK and CDK4/6 inhibitors in vitro and in vivo in KRAS mutant colorectal cancer models; Oncotarget 39595
4) Gong et al. (2017), MEK162 Enhances Antitumor Activity of 5-Fluorouracil and Trifluridine in KRAS-mutated Human Colorectal Cancer Cell Lines; Anticancer Res. 37 2831
5) Van Cutsem et al. (2019), Binimetinib, Encorafenib, and Cetuximab Triplet Therapy for Patients With BRAF V600E-Mutant Metastatic Colorectal Cancer: Safety Lead-In Results From Phase III BEACON Colorectal Cancer study; J. Clin. Oncol. 180 2459

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Catalog#  10-4789-0005

$39.00
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Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee.
 
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CAS:
606143-89-9
Catalog Number:
10-4789
Activity:
MEK1/2 inhibitor
Chemical Name:
6-(4-Bromo-2-fluoroanilino)-7-fluoro-N-(2-hydroxyethoxy)-3-methylbenzimidazole-5-carboxamide
Alternate Names:
ARRY-162; MEK162
Molecular Weight:
441.23
Molecular Formula:
C17H15BrF2N4O3
Solubility:
Soluble in DMSO (up to at least 25 mg/ml)
Physical Properties:
White solid
Purity:
99% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C (des.)
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

Focus BiomoleculesPlymouth Meeting, PA USA1-855-FOCUS21

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