Binimetinib NEW
| Price | $35 | $57 | $68 |
| Package | 5mg | 10mg | 25mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-18 |
Product Details
| Product Name: Binimetinib | CAS No.: 606143-89-9 |
| Purity: 99% | Supply Ability: 10g |
| Release date: 2024/11/18 |
Product Introduction
Bioactivity
| Name | Binimetinib |
| Description | Binimetinib (ARRY-162) is a MEK1/2 inhibitor (IC50=12 nM) with selective and oral activity. Binimetinib has antitumor activity for the treatment of metastatic melanoma that cannot be resected or has a BRAF V600E or V600K mutation. |
| Cell Research | MEK162 is dissolved in DMSO and stored, and then diluted with appropriate medium before use[2]. MCF7 cells infected as indicated are seeded in 12-well plates (2×104). After 24 hours, cells are treated with BEZ235 (100 or 200 nM), BKM120 (0.75 or 1 μM), GDC-0941 (1 μM), or MK2206 (2 μM) alone or in combination with MEK162 (1 μM), BI-D1870 (10 μM), or AZD6244 (1 μM), as indicated in text. Cell numbers are quantified by fixing cells with 4% glutaraldehyde or methanol, washing the cells twice in Water, and staining the cells with 0.1% crystal violet. The dye is subsequently extracted with 10% acetic acid, and its absorbance is determined (570 nm). Growth curves are performed in triplicate. Viability assays with CellTiter-Glo are performed by plating 2,000 cells in 96-well plates, adding the drug at 24 hours, and assaying 4 to 5 days after drug addition. Cell-cycle and hypodiploid apoptotic cells are quantified by flow cytometry. Briefly, cells are washed with PBS, fixed in cold 70% ethanol, and then stained with propidium iodide while being treated with RNase. Quantitative analysis of sub-G1 cells is carried out in a FACScalibur cytometer using Cell Quest software[2]. |
| In vitro | In models of collagen-induced arthritis (CIA) and adjuvant-induced arthritis (AIA) in rats, ARRY-438162 demonstrated significant anti-inflammatory effects. At doses of 1/3 mg/kg administered twice daily orally (p.o.), ARRY-438162 reduced ankle diameter swelling by 27%/50% in the CIA model, outperforming ibuprofen's 46% reduction. Higher doses of 3/10 mg/kg showed 11%/34% inhibition of ankle swelling in the AIA model. Moreover, in immunodeficient mice injected with MCF7-RSK4 cells, the combination of ARRY-438162 (6 mg/kg, twice daily) with BEZ235 significantly diminished tumor growth. In the AIA rat model, ARRY-438162 (10 mg/kg) completely suppressed serum IL-6 concentrations in a dose-dependent manner compared to controls. Similarly, in both CIA and AIA rat models, administration of ARRY-438162 (10 mg/kg, twice daily p.o.) dose-dependently ameliorated disease severity. The same dosing regimen significantly mitigated lesions (inflammation, cartilage damage, angiogenesis, and bone resorption) in the CIA model, with 1/3 mg/kg doses inhibiting these effects by 32% and 60%, respectively. Furthermore, in the AIA rat model, ARRY-438162 at 10/30 mg/kg doses significantly and dose-dependently reduced ankle swelling compared to control groups. |
| In vivo | ARRY-438162 is an ATP non-competitive inhibitor for MEK1/2, capable of inhibiting intracellular pERK with an IC50 of 11 nM. When used in combination, MEK162 (1 μM) and MK-2206 (2 μM) can fully reverse the resistance of MCF7 cells expressing RSK. ARRY-438162 at 2 μM exhibits minimal impact on osteoblast differentiation. At a concentration of 10 μM, ARRY-438162 inhibits osteoclast resorption in vitro with an IC50 of 625 nM. Additionally, ARRY-438162 at 625 nM suppresses osteoclast differentiation in vitro with an IC50 of 39 nM. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 50 mg/mL (113.32 mM) Ethanol : < 1 mg/mL (insoluble or slightly soluble) H2O : < 1 mg/mL (insoluble or slightly soluble) |
| Keywords | Inhibitor | MEK-162 | Mitogen-activated protein kinase kinase | MEK 162 | ARRY 162 | ARRY162 | ARRY438162 | MAPKK | MAP2K | Binimetinib | ARRY 438162 | inhibit | Autophagy | MEK |
| Inhibitors Related | Stavudine | Xylitol | Myricetin | Sodium 4-phenylbutyrate | Hydroxychloroquine | Guanidine hydrochloride | Taurine | Curcumin | Oxyresveratrol | Paeonol | Naringin | Gefitinib |
| Related Compound Libraries | 疼痛相關(guān)化合物庫 | 經(jīng)典已知活性庫 | EMA 上市藥物庫 | 激酶抑制劑庫 | 抗癌臨床化合物庫 | 抑制劑庫 | FDA 上市藥物庫 | 已知活性化合物庫 | 抗癌藥物庫 | 抗癌活性化合物庫 |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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