MEK162 (ARRY-162, ARRY-438162)MEK1/2 inhibitor,potent and selective CAS# 606143-89-9 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
Cas No. | 606143-89-9 | SDF | Download SDF |
PubChem ID | 10288191 | Appearance | Powder |
Formula | C17H15BrF2N4O3 | M.Wt | 441.23 |
Type of Compound | N/A | Storage | Desiccate at -20°C |
Synonyms | Binimetinib; ARRY-162; ARRY-438162 | ||
Solubility | DMSO : 50 mg/mL (113.32 mM; Need ultrasonic) | ||
Chemical Name | 6-(4-bromo-2-fluoroanilino)-7-fluoro-N-(2-hydroxyethoxy)-3-methylbenzimidazole-5-carboxamide | ||
SMILES | CN1C=NC2=C1C=C(C(=C2F)NC3=C(C=C(C=C3)Br)F)C(=O)NOCCO | ||
Standard InChIKey | ACWZRVQXLIRSDF-UHFFFAOYSA-N | ||
Standard InChI | InChI=1S/C17H15BrF2N4O3/c1-24-8-21-16-13(24)7-10(17(26)23-27-5-4-25)15(14(16)20)22-12-3-2-9(18)6-11(12)19/h2-3,6-8,22,25H,4-5H2,1H3,(H,23,26) | ||
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. |
Description | MEK162 is a potent inhibitor of MEK1/2 with IC50 value of 12 nM. | |||||
Targets | MEK1 | MEK2 | ||||
IC50 | 12 nM | 12 nM |
MEK162 (ARRY-162, ARRY-438162) Dilution Calculator
MEK162 (ARRY-162, ARRY-438162) Molarity Calculator
1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
1 mM | 2.2664 mL | 11.332 mL | 22.6639 mL | 45.3278 mL | 56.6598 mL |
5 mM | 0.4533 mL | 2.2664 mL | 4.5328 mL | 9.0656 mL | 11.332 mL |
10 mM | 0.2266 mL | 1.1332 mL | 2.2664 mL | 4.5328 mL | 5.666 mL |
50 mM | 0.0453 mL | 0.2266 mL | 0.4533 mL | 0.9066 mL | 1.1332 mL |
100 mM | 0.0227 mL | 0.1133 mL | 0.2266 mL | 0.4533 mL | 0.5666 mL |
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. |
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MEK162 (ARRY-162, ARRY-438162) is a novel, selective inhibitor of MEK 1/2 with IC50 of about 12 nM [1].
Co-treatment of MEK162 and PKC inhibitors persistently inhibited MAP-kinase pathway. The co-treatment can halt proliferation and induce apoptosis of uveal melanoma cells even with GNAQ or GNA11 mutations [2]. All N-RAS mutant melanoma cells were sensitive to MEK 162. MEK162 reduced ERK1/2 phosphorylation, clonogenic survival, and induced apoptosis [3].
Phase Ib or II clinical trials were conducted in 32 cutaneous melanoma patients. 20 patients in MEK162 monotherapy and 12 on MEK162 plus RAF inhibitor or selective BRAF inhibitor combination therapy underwent ophthalmological examinations and multimodal imaging. These therapy all induced transient retinopathy with multiple bilateral lesions in some patients. The effect of MEK162 in retinopathy has been usually mild, self-limiting, and tolerable [4].
References:
[1]. Jed Pheneger, Eli Wallace, Allison Marlow, Brian Hurley, Joe Lyssikatos, Alison M. Bendele, Patrice A. Lee1. Array BioPharma, Boulder, CO; Bolder BioPath, Boulder, CO. Characterization of ARRY-438162, a potent MEK inhibitor in combination with Methotrexate or Ibuprofen in vivo models of arthritis. American college of rheumatology. 2006 Annual Scientific Meeting.
[2]. Chen X, Wu Q, Tan L, Porter D, Jager MJ, Emery C, Bastian BC. Combined PKC and MEK inhibition in uveal melanoma with GNAQ and GNA11 mutations. Oncogene. 2013 Oct 21.
[3]. Thumar J, Shahbazian D, Aziz SA, Jilaveanu LB, Kluger HM. MEK targeting in N-RAS mutated metastatic melanoma. Mol Cancer. 2014 Mar 4;13:45.
[4]. Urner-Bloch U, Urner M, Stieger P, Galliker N, Winterton N, Zubel A, Moutouh-de Parseval L, Dummer R, Goldinger SM. Transient MEK inhibitor-associated retinopathy in metastatic melanoma. Ann Oncol. 2014 May 26. pii: mdu169.
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