Binimetinib | MEK1/2 inhibitor

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
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Available Options

Size:PriceQuantity 
5 mg$39.00
25 mg$115.00

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

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
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. 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