1H-Benzimidazole-6-carboxamide, 5-[(4-bromo-2-fluorophenyl)amino]-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-
Binimetinib
CAS: 606143-89-9
Molecular Formula: C17H15BrF2N4O3
1H-Benzimidazole-6-carboxamide, 5-[(4-bromo-2-fluorophenyl)amino]-4-fluoro-N-(2-hydroxyethoxy)-1-methyl- - Names and Identifiers
1H-Benzimidazole-6-carboxamide, 5-[(4-bromo-2-fluorophenyl)amino]-4-fluoro-N-(2-hydroxyethoxy)-1-methyl- - Physico-chemical Properties
| Molecular Formula | C17H15BrF2N4O3 |
| Molar Mass | 441.23 |
| Density | 1.67 |
| Melting Point | >203oC (dec.) |
| Solubility | Soluble in DMSO (up to at least 25 mg/ml) |
| Appearance | solid |
| Color | White |
| pKa | 14.20±0.10(Predicted) |
| Storage Condition | -20°C |
| Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. |
| In vitro study | ARRY-438162(625 nM) inhibited the differentiation of osteoclasts in vitro, IC50 was 39 nM. ARRY-438162(10 M) inhibition of osteoclast resorption in vitro, IC50 was 625 nM. ARRY-438162(2 M) weak effect on osteoblast differentiation. ARRY-438162 is a recently disclosed potent, selective, ATP non-competitive MEK1/2 inhibitor that acts on cells to inhibit pERK with an IC50 of 11 nM. MEK162 (1 μm) in combination with MK-2206 (2 μm) completely reversed the resistance of MCF7 cells expressing RSK. ARRY-438162(625 nM) inhibited osteoclast differentiation in vitro with IC50 of 39 nM. ARRY-438162(10 M) inhibition of osteoclast resorption in vitro, IC50 was 625 nM. ARRY-438162(2 M) weak effect on osteoblast differentiation. ARRY-438162 is a recently disclosed potent, selective, ATP non-competitive MEK1/2 inhibitor that acts on cells to inhibit pERK with an IC50 of 11 nM. MEK162 (1 μm) in combination with MK-2206 (2 μm) completely reversed the resistance of MCF7 cells expressing RSK. |
| In vivo study | ARRY-438162 rats with collagen-induced arthritis (CIA) and adjuvant-induced arthritis (AIA) were treated orally at a dose of 10 mg/kg twice a day to reduce the severity of the disease, this effect is dose-dependent. ARRY-438162 according to the dose of 1 mg/kg and 3 mg/kg oral treatment of rat collagen induced arthritis (CIA) model, twice a day, inhibit the increase of ankle joint diameter, respectively, 27% and 50%, treatment with Ibuprofen, on the other hand, inhibited by 46%. ARRY-438162 at a dose of 10 mg/kg oral treatment of rat collagen induced arthritis (CIA) model, twice a day, significantly inhibit the lesions (inflammation, cartilage damage, pannus formation, and bone resorption), treatment at 1 mg/kg and 3 mg/kg resulted in 32% and 60% inhibition, respectively. ARRY-438162 treatment of 3 mg/kg and 10 mg/kg doses in the rat model of adjuvant-induced arthritis (AIA) inhibited the diameter of the ankle joint by 11% and 34%, respectively. ARRY-438162 treatment of the rat adjuvant-induced arthritis (AIA) model at doses of 10 mg/kg and 30 mg/kg significantly inhibited ankle joint swelling compared with the control group, and this effect was dose-related. ARRY-438162 treatment of the rat adjuvant-induced arthritis (AIA) model at a dose of 10 mg/kg completely inhibited the serum concentration by IL-6 compared with the control group, which was dose-related. ARRY-438162 the rat adjuvant-induced arthritis (AIA) model treated at a dose of 30 mg/kg, compared with the control group, inhibited the relative spleen weight, significantly inhibited bone resorption and inflammation, and this effect was dose-related. Treatment of immunodeficient mice injected with ARRY-438162 cells with MCF7-RSK4 (6 mg/kg twice daily) in combination with BEZ235 significantly reduced tumor growth. ARRY-438162 rats with collagen-induced arthritis (CIA) and adjuvant-induced arthritis (AIA) were treated orally at a dose of 10 mg/kg twice a day to reduce the severity of the disease, this effect is dose-dependent. ARRY-438162 according to the dose of 1 mg/kg and 3 mg/kg oral treatment of rat collagen induced arthritis (CIA) model, twice a day, inhibit the increase of ankle joint diameter, respectively, 27% and 50%, treatment with Ibuprofen, on the other hand, inhibited by 46%. ARRY-438162 at a dose of 10 mg/kg oral treatment of rat collagen induced arthritis (CIA) model, twice a day, significantly inhibit the lesions (inflammation, cartilage damage, pannus formation, and bone resorption), treatment at 1 mg/kg and 3 mg/kg resulted in 32% and 60% inhibition, respectively. ARRY-438162 treatment of 3 mg/kg and 10 mg/kg doses in the rat model of adjuvant-induced arthritis (AIA) inhibited the diameter of the ankle joint by 11% and 34%, respectively. ARRY-438162 treatment of the rat adjuvant-induced arthritis (AIA) model at doses of 10 mg/kg and 30 mg/kg significantly inhibited ankle joint swelling compared with the control group, and this effect was dose-related. ARRY-438162 treatment of the rat adjuvant-induced arthritis (AIA) model at a dose of 10 mg/kg completely inhibited the serum concentration by IL-6 compared with the control group, which was dose-related. ARRY-438162 the rat adjuvant-induced arthritis (AIA) model treated at a dose of 30 mg/kg, compared with the control group, inhibited the relative spleen weight, significantly inhibited bone resorption and inflammation, and this effect was dose-related. Treatment of immunodeficient mice injected with ARRY-438162 cells with MCF7-RSK4 (6 mg/kg twice daily) in combination with BEZ235 significantly reduced tumor growth. |
1H-Benzimidazole-6-carboxamide, 5-[(4-bromo-2-fluorophenyl)amino]-4-fluoro-N-(2-hydroxyethoxy)-1-methyl- - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.266 ml | 11.332 ml | 22.664 ml |
| 5 mM | 0.453 ml | 2.266 ml | 4.533 ml |
| 10 mM | 0.227 ml | 1.133 ml | 2.266 ml |
| 5 mM | 0.045 ml | 0.227 ml | 0.453 ml |
Last Update：2024-01-02 23:10:35
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Product Name: MEK162 (ARRY-162, ARRY-438162) Visit Supplier Webpage Request for quotation
CAS: 606143-89-9
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CAS: 606143-89-9
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
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Product Name: MEK162 (ARRY-162, ARRY-438162) Visit Supplier Webpage Request for quotation
CAS: 606143-89-9
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 606143-89-9
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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