Details of the Active Pharmaceutical Ingredient (API)

General Information of API (ID: D00883)
Name
Binimetinib
Synonyms    Click to Show/Hide the Synonyms of This API
Binimetinib; 606143-89-9; MEK162; ARRY-162; ARRY-438162; 5-[(4-Bromo-2-fluorophenyl)amino]-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-1H-benzimidazole-6-carboxamide; MEK-162; Mektovi; ARRY 162; ARRY 438162; UNII-181R97MR71; Binimetinib (MEK-162); MEK162 (ARRY-162, ARRY-438162); NVP-MEK162; Binimetinib (MEK162, ARRY-162, ARRY-438162); 181R97MR71; 6-(4-bromo-2-fluoroanilino)-7-fluoro-N-(2-hydroxyethoxy)-3-methylbenzimidazole-5-carboxamide; 5-((4-bromo-2-fluorophenyl)amino)-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-1H-benzo[d]imidazole-6-carboxamide.; 5-(4-Bromo-2-fluoroanilino)-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-1H-benzimidazole-6-carboxamide; Binimetinib [USAN:INN]; binimetinibum; Mektovi (TN); ARRY-162; ARRY-438162; MEK 162; ARRY 162; ARRY 438162; Mek162, Binimetinib; MEK162(Binimetinib); Binimetinib (JAN/USAN); cc-455; MLS006011180; C17H15BrF2N4O3; SCHEMBL570088; GTPL7921; CHEMBL3187723; MEK162 (Arry-162); AMY9056; AOB2072; DTXSID70209422; QCR-138; ARRY-162,MEK-162; CHEBI:145371; HMS3652J14; HMS3747G09; BCP06780; EX-A1024; MFCD22124525; NSC764042; NSC788187; NSC799361; s7007; ZINC38460704; AKOS026750517; CCG-269133; CS-0627; DB11967; NSC-764042; NSC-788187; NSC-799361; SB16501; NCGC00345804-01; NCGC00345804-10; 1073666-70-2; 6-(4-bromo-2-fluorophenylamino)-7-fluoro-N-(2-hydroxyethoxy)-3-methyl-3H-benzo[d]imidazole-5-carboxamide; AC-29023; AK175886; AS-16706; DA-35030; HY-15202; SMR004702949; cas:606143-89-9;MEK162; AB0095018; FT-0697088; SW219910-1; Y1468; A11493; D10604; W-5894; Binimetinib;MEK-162; ARRY-162;ARRY-438162; J-516581; Q19903515; 5-[(4-bromo-2-fluorophenyl)amino]-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-1H-1,3-benzodiazole-6-carboxamide; 5-[(4-Bromo-2-Fluorophenyl)Amino]-4-Fluoro-N-(2-Hydroxyethoxy)-1-Methyl-1H-Benzimidazole-6-Carboxami; 6-(4-bromo-2-fluorophenylamino)-7-fluoro-3-methyl-3H-benzoimidazole-5-carboxylic acid (2-hydroxyethyoxy)-amide; 6-[(4-bromo-2-fluorophenyl)amino]-7-fluoro-N-(2-hydroxyethoxy)-3-methylbenzimidazole-5-carboxamide; N-(2-hydroxyethoxy)-4-fluoro-5-(2-fluoro-4-bromophenylamino)-1-methyl-1H-benzoimidazole-6-carboxamide; QO7
Clinical Status
Approved
PubChem CID
10288191
Formula
C17H15BrF2N4O3
Canonical SMILES
CN1C=NC2=C1C=C(C(=C2F)NC3=C(C=C(C=C3)Br)F)C(=O)NOCCO
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)
InChIKey
ACWZRVQXLIRSDF-UHFFFAOYSA-N
   Click to Show/Hide the Molecular Data (Structure/Property) of This API
Structure
<iframe style="width: 300px; height: 300px;" frameborder="0" src="https://embed.molview.org/v1/?mode=balls&cid=10288191"></iframe>
3D MOL 2D MOL
Physicochemical Properties Molecular Weight 441.2 Topological Polar Surface Area 88.4
XlogP 3.1 Complexity 521
Heavy Atom Count 27 Rotatable Bond Count 6
Hydrogen Bond Donor Count 3 Hydrogen Bond Acceptor Count 7
Full List of Drug Formulations (DFMs) Containing This API
          Binimetinib 15 mg tablet Click to Show/Hide the Full List of Formulation(s):          1 Formulation(s)
             Drug Formulation 1 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Lactose Monohydrate; Microcrystalline Cellulose; Croscarmellose Sodium; Magnesium Stearate (Vegetable Source); Colloidal Silicon Dioxide; Polyvinyl Alcohol; Polyethylene Glycol; Titanium Dioxide; Talc; Ferric Oxide Yellow; Ferrosoferric Oxide
                   Dosage Form Tablet
                   Company Array Biopharma
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Polyvinyl alcohol DIG Info Debrisoquine 4-hydroxylase (EC50 = 354.8 uM) [1]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [2]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [2]
Polyethylene glycol 4000 DIG Info Albendazole monooxygenase (Inhibition ratio < 40 %) [3]
References
1 Mediation of in vitro cytochrome p450 activity by common pharmaceutical excipients. Mol Pharm. 2013 Jul 1;10(7):2739-48.
2 Effects of commonly used excipients on the expression of CYP3A4 in colon and liver cells. Pharm Res. 2010 Aug;27(8):1703-12.
3 Pharmaceutical excipients inhibit cytochrome P450 activity in cell free systems and after systemic administration. Eur J Pharm Biopharm. 2008 Sep;70(1):279-88.

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