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Products are for research use only. Not for human use. We do not sell to patients.

Signaling Pathway

MEK162

HY-15202

(Binimetinib; ARRY-162; ARRY-438162; MEK 162; ARRY 162; ARRY 438162)

MEK162

MEK162 Chemical Structure

MEK162(ARRY-438162; ARRY-162) is a potent inhibitor of MEK1/2 with IC50 of 12 nM.

Price and Availability of MEK162

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Size Price Stock Quantity
10 mM * 1 mL $66 In-stock
10 mg $60 In-stock
50 mg $140 In-stock
100 mg $230 In-stock
200 mg Get quote
500 mg Get quote
Size Price Stock Quantity
10 mM * 1 mL €65 In-stock
10 mg €59 In-stock
50 mg €137 In-stock
100 mg €225 In-stock
200 mg Get quote
500 mg Get quote

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MEK162 Data Sheet

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    Purity: 98.69%

  • Pdf Version Network Version

    DataSheet

    Pdf Version Network Version

    MSDS

    Pdf Version

    COA

Related Compound Libraries

Inhibitor Kit

Biological Activity of MEK162

MEK162(ARRY-438162; ARRY-162) is a potent inhibitor of MEK1/2 with IC50 of 12 nM.
IC50 value: 12 nM [1]
Target: MEK1/2
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. [2] ARRY-438162 is a recently disclosed potent and selective ATP non-competitive MEK1/2 inhibitor, inhibits pERK in cells with an IC50 of11 nM. [3] MEK162 (1 μM) combined with MK-2206 (2 μM) completely reverses the resistance of RSK-expressing MCF7 cells. [4]
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 [1]. MEK162 (6 mg/kg, BID) combined with BEZ235 results in a significant reduction of tumor growth in immunodeficient mice injected with MCF7 cells [4].

Chemical Information

M.Wt 441.23 Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Formula C17H15BrF2N4O3
CAS No 606143-89-9
Solvent & Solubility

in DMSO > 10 mM

Preparing Stock Solutions

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

Clinical Information of MEK162

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

References on MEK162

  • Related MEK Products

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    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

    AZD8330(ARRY-424704; ARRY-704) is a novel, selective, non-ATP competitive MEK 1/2 inhibitor with IC50 of 7 nM.

  • BIX02188

    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

    BIX02189 is a selective MEK5/ERK5 inhibitor with an IC50 of 59 nM.

  • CI-1040

  • GDC-0623

    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

    MEK inhibitor is a potent MEK inhibitor, antitumor agent.

  • PD0325901

  • PD318088

    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

    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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