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Products are for research use only. Not for human use. We do not sell to patients.
(Binimetinib; ARRY-162; ARRY-438162; MEK 162; ARRY 162; ARRY 438162)
MEK162 Chemical Structure
Protease Inhibitor Cocktail
protease inhibitor cocktails are used in mammalian cell lysates or tissue extracts to increase protein stability.
MEK162(ARRY-438162; ARRY-162) is a potent inhibitor of MEK1/2 with IC50 of 12 nM.
IC50 value: 12 nM 
in vitro: ARRY-438162 (625 nM) inhibits in vitro osteoclast differentiation with IC50 of 39 nM. ARRY-438162 (10 μM) inhibits in vitro osteoclast resorption with IC50 of 625 nM. ARRY-438162 (2 μM) weakly affects osteoblast differentiation.  ARRY-438162 is a recently disclosed potent and selective ATP non-competitive MEK1/2 inhibitor, inhibits pERK in cells with an IC50 of11 nM.  MEK162 (1 μM) combined with MK-2206 (2 μM) completely reverses the resistance of RSK-expressing MCF7 cells. 
in vivo: ARRY-438162 (10 mg/kg, po, bid) reduces disease severity in a dose-related manner in rat collagen-induced arthritis (CIA) and rat adjuvant-induced arthritis (AIA) models. ARRY-438162 (po, bid) inhibits increases in ankle diameter by 27% and 50% at 1 mg/kg and 3 mg/kg in the rat collagen-induced arthritis (CIA) model, while ibuprofen has 46% inhibition. ARRY-438162 (10 mg/kg, po, bid) significantly inhibits lesions (inflammation, cartilage damage, pannus formation and bone resorption) by 32% and 60% at 1 mg/kg and 3 mg/kg in the rat collagen-induced arthritis (CIA) model. ARRY-438162 inhibits AIA ankle diameter 11% and 34% at 3 mg/kg and 10 mg/kg in rat adjuvant-induced arthritis (AIA) models . MEK162 (6 mg/kg, BID) combined with BEZ235 results in a significant reduction of tumor growth in immunodeficient mice injected with MCF7 cells .
|M.Wt||441.23||Storage||Please store the product under the recommended conditions in the Certificate of Analysis.|
|Solvent & Solubility||
in DMSO > 10 mM
|1 mg||5 mg||10 mg|
|1 mM||2.2664 mL||11.3320 mL||22.6639 mL|
|5 mM||0.4533 mL||2.2664 mL||4.5328 mL|
|10 mM||0.2266 mL||1.1332 mL||2.2664 mL|
|Product Name||Sponsor Only||Condition||Start Date||End Date||Phase||Last Change Date|
|MEK162||Novartis AG||Stage IV melanoma||30-SEP-13||30-JUN-17||Phase 3||05-NOV-13|
|Novartis AG||Stage IV melanoma||31-JUL-13||31-MAY-16||Phase 3||07-SEP-13|
|Novartis AG||Hematological neoplasm||30-SEP-13||31-AUG-17||Phase 2||26-NOV-13|
|Novartis AG||Stage III melanoma||31-JUL-13||31-MAY-16||Phase 3||07-SEP-13|
|Novartis AG||Stage IV melanoma||30-SEP-13||31-OCT-16||Phase 2||06-NOV-13|
AS703026(Pimasertib) is a highly selective, potent, ATP non-competitive allosteric inhibitor of MEK1/2 with IC50 of 5 nM-2 (mu)M in MM cell lines.
AZD8330(ARRY-424704; ARRY-704) is a novel, selective, non-ATP competitive MEK 1/2 inhibitor with IC50 of 7 nM.
BIX02188 is a selective inhibitor of MEK5 with IC50 of 4.3 nM, also inhibits ERK5 catalytic activity with IC50 of 810 nM, and does not inhibit closely related kinases MEK1, MEK2, ERK2, and JNK2.
BIX02189 is a selective MEK5/ERK5 inhibitor with an IC50 of 59 nM.
GDC-0623 is a potent, ATP-uncompetitive inhibitors of MEK1(Ki=0.13 nM, (addition)ATP); 6-fold weaker potency against HCT116 (KRAS(G13D), EC50=42 nM) versus A375 (BRAF(V600E), EC50=7 nM).
MEK inhibitor is a potent MEK inhibitor, antitumor agent.
PD318088 is a non-ATP competitive allosteric MEK1/2 inhibitor, binds simultaneously with ATP in a region of the MEK1 active site that is adjacent to the ATP-binding site.
PD98059 is a non-ATP competitive MEK inhibitor with IC50 of 2 (mu)M, specifically inhibits MEK-1-mediated activation of MAPK; does not directly inhibit ERK1 or ERK2.
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