Binimetinib(ARRY-162,MEK162)| MEK1/2 inhibitor

Cas No.:	606143-89-9
Chemical Name:	1H-Benzimidazole-6-carboxamide,5-[(4-bromo-2-fluorophenyl)amino]-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-
Synonyms:	ARRY 162; ARRY 438162, MEK-162,Binimetinib;MEK-162; ARRY-162; ARRY-438162
SMILES:	CN1C=NC2=C1C=C(C(=C2F)NC3=C(C=C(C=C3)Br)F)C(=O)NOCCO
Formula:	C₁₇H₁₅BrF₂N₄O₃
M.Wt:	441.23
Sotrage:	2 years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSO

Description:	Binimetinib (MEK162) is an oral and selective MEK1/2 inhibitor with an IC50 of 12 nM.
In Vivo:	Treatment with Binimetinib (ARRY-438162) reduces disease severity in a dose-related manner in both animal models. ARRY-438162 in the CIA model inhibits increases in ankle diameter by 27% and 50% at 1 and 3 mg/kg, while Ibuprofen has 46% inhibition. When combined with Ibuprofen, these same two doses result in 74% and 72% inhibition, respectively. Microscopic examination of the ankle joints show Binimetinib (ARRY-438162) significantly inhibits lesions (inflammation, cartilage damage, pannus formation and bone resorption) by 32% and 60% at 1 and 3 mg/kg, while treatment with Ibuprofen alone results in 17% inhibition, which is not significantly different from the controls. When these two doses of Binimetinib (ARRY-438162) are combined with ibuprofen, the result is 54% and 77% inhibition of joint destruction. In AIA, 3 and 10 mg/kg of Binimetinib (ARRY-438162) inhibit AIA ankle diameter 11% and 34%, while MTX has 33% inhibition. When combined with MTX, 3 and 10 mg/kg of Binimetinib (ARRY-438162) result in 55% and 71% inhibition. Microscopic examination of ankle joints for inflammation and bone resorption also shows improved efficacy versus either compound alone[1]. When Binimetinib (MEK162) is combined with BEZ235, a significant reduction of tumor growth is observed (P=0.01). This increase in antitumor activity is accompanied by a decrease in phospho-ERK and phospho-S6 staining. No significant changes are observed in phospho-4EBP1 staining, a direct target of mTOR activity[2].
In Vitro:	In MCF7 cells, RSK3 or RSK4 expression decreases response to treatment with any of the PI3K inhibitors alone. However, the combination of PI3K inhibition with Binimetinib (MEK162) or BI-D1870 completely reverses the resistance of RSK-expressing cells[2]. Binimetinib (MEK162) blocks basal ERK phosphorylation in all HRAS mutant cell lines. The combination of Everolimus and AZD6244/MEK162 causes a stronger inhibition of S6 kinase than single use of Everolimus on Western blot. The combination of Everolimus and AZD6244/MEK162 also translated in a stronger blockade of cell growth in HRAS mutant cells than single use. Binimetinib (MEK162) shows stronger synergism with Everolimus than AZD6244[3].

Cat. No.	Product name	Field of application
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DC75721	CL2A-SN38 (Govitecan)	CL2A-SN38 is a SN38 derivative with a peptide-linker which can easily react with antibody to form an antibody-drug conjugate (ADC). CL2A-SN-38 is composed of a potent a DNA Topoisomerase I inhibitor SN-38 and a linker CL2A to make antibody drug conjugate (ADC). CL2A-SN-38 provides significant and specific antitumor effects against a range of human solid tumor types. CL2A is a noncleavable complicated PEG8- and triazole-containing PABC-peptide-mc linker. CL2A is cleavable through pH sensitivity, giving rise to bystander effect, and binds the antibody at a cysteine residue via a disulfide bond. .
DC47877	tri-GalNAc-COOH (acetylation)	tri-GalNAc-COOH acetylation is the acetylated and modified form of tri-GalNAc-COOH. tri-GalNAc-COOH acetylation can be used for the synthesis of LYTAC.
DC46965	Tri-GalNAc-COOH	tri-GalNAc-COOH is an asialoglycoprotein receptor (ASGPR) ligand that can be used for LYsosome TArgeting Chimera (LYTAC) research.
DC46471	RP101988	RP101988, the major active metabolite of Ozanimod, is a selective, potent S1PR1 (sphingosine-1-phosphate receptor 1) agonist, with EC50s of 0.19 nM and 32.8 nM for S1PR1 and S1PR5, respectivlely.
DC37901	PD-173212	PD-173212 is a small molecule N-type calcium channel blocker.
DC37333	N,N-Diethyl-p-toluamide	N,N-Diethyl-p-toluamide is a mosquito repellent.
DC37321	AI3-15902	AI3-15902 is a biochemical.
DC37283	Methyl phenylcarbamate	Methyl phenylcarbamate is a biochemical.
DC37252	Ampyrone	Ampyrone is a metabolite of AMINOPYRINE with analgesic and anti-inflammatory properties. It is used as a reagent for biochemical reactions producing peroxides or phenols. Ampyrone stimulates LIVER MICROSOMES and is also used to measure extracellular water.

MEK162(Binimetinib)