Name: Binimetinib (MEK-162)
CAS#: 606143-89-9
Chemical Formula: C17H15BrF2N4O3
Exact Mass: 440.02956
Molecular Weight: 441.22681
Elemental Analysis: C, 46.28; H, 3.43; Br, 18.11; F, 8.61; N, 12.70; O, 10.88
EOS Med Chem produce Binimetinib (MEK-162),606143-89-9 in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.
Binimetinib (MEK-162),606143-89-9 Intermediates, EOS Med Chem have 8; Binimetinib (MEK-162),606143-89-9 Impurity we have 10, all from GMP, FDA plant.
Now Binimetinib (MEK-162),606143-89-9 DMF document is preparing.
Until 2016, Aug, Binimetinib (MEK-162),606143-89-9 more than produced 25kg API, 120kg Intermediates
GMP PRODUCE:
Alectinib;Veliparib;Acalabrutinib;Venetoclax;Sotagliflozin;Ledipasvir;LX1606;Anacetrapib;Abemaciclib
Binimetinib Binimetinib 606143-89-9
Binimetinib Intermediates MEK-162; ARRY-162; ARRY-438162; 606143-89-9
Binimetinib Intermediates Methyl 4-amino-2-((4-bromo-2-fluorophenyl)amino)-3-fluoro-5-nitrobenzoate
Binimetinib Intermediates Methyl 6-((4-bromo-2-fluorophenyl)amino)-7-fluoro-1H-benzo[d]imidazole-5-carboxylate 606143-48-0
Binimetinib Intermediates 5-((4-bromo-2-fluorophenyl)amino)-4-fluoro-1-methyl-1H-benzo[d]imidazole-6-carboxylic acid 1415564-99-6
Binimetinib Intermediates Methyl 5-((4-bromo-2-fluorophenyl)amino)-4-fluoro-1-methyl-1H-benzo[d]imidazole-6-carboxylate 1415559-93-1
Description: Binimetinib, also known as MEK162 (ARRY-162), is an oral, highly selective MEK inhibitor. In preclinical studies, MEK162 showed significant antitumor activities in cell lines and animal models. MEK162 is the first targeted therapy to show activity in patients with NRAS -mutated melanoma and might offer a new option for a cancer with few effective treatments.
Synonym: MEK162; MEK-162; MEK 162; ARRY162; ARRY-162; ARRY 162; ARRY438162, Binimetinib
IUPAC/Chemical Name: 5-((4-bromo-2-fluorophenyl)amino)-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-1H-benzo[d]imidazole-6-carboxamide.
SMILES Code: O=C(C1=C(NC2=CC=C(Br)C=C2F)C(F)=C3N=CN(C)C3=C1)NOCCO
1: Hamidi H, Lu M, Chau K, Anderson L, Fejzo M, Ginther C, Linnartz R, Zubel A, Slamon DJ, Finn RS. KRAS mutational subtype and copy number predict in vitro response of human pancreatic cancer cell lines to MEK inhibition. Br J Cancer. 2014 Aug 28. doi: 10.1038/bjc.2014.475. [Epub ahead of print] PubMed PMID: 25167228.
2: Rebecca VW, Alicea GM, Paraiso KH, Lawrence H, Gibney GT, Smalley KS. Vertical inhibition of the MAPK pathway enhances therapeutic responses in NRAS-mutant melanoma. Pigment Cell Melanoma Res. 2014 Aug 11. doi: 10.1111/pcmr.12303. [Epub ahead of print] PubMed PMID: 25130256.
3: 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 Jul;25(7):1437-41. doi: 10.1093/annonc/mdu169. Epub 2014 May 26. PubMed PMID: 24864047.
4: Küsters-Vandevelde HV, Willemsen AE, Groenen PJ, Küsters B, Lammens M, Wesseling P, Djafarihamedani M, Rijntjes J, Delye H, Willemsen MA, van Herpen CM, Blokx WA. Experimental treatment of NRAS-mutated neurocutaneous melanocytosis with MEK162, a MEK-inhibitor. Acta Neuropathol Commun. 2014 Apr 8;2(1):41. doi: 10.1186/2051-5960-2-41. PubMed PMID: 24713450; PubMed Central PMCID: PMC4023633.
5: 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. doi: 10.1186/1476-4598-13-45. PubMed PMID: 24588908; PubMed Central PMCID: PMC3945937.
6: Gritsman K, Yuzugullu H, Von T, Yan H, Clayton L, Fritsch C, Maira SM, Hollingworth G, Choi C, Khandan T, Paktinat M, Okabe RO, Roberts TM, Zhao JJ. Hematopoiesis and RAS-driven myeloid leukemia differentially require PI3K isoform p110α. J Clin Invest. 2014 Apr 1;124(4):1794-809. doi: 10.1172/JCI69927. Epub 2014 Feb 24. PubMed PMID: 24569456; PubMed Central PMCID: PMC3973083.
7: Miller CR, Oliver KE, Farley JH. MEK1/2 inhibitors in the treatment of gynecologic malignancies. Gynecol Oncol. 2014 Apr;133(1):128-37. doi: 10.1016/j.ygyno.2014.01.008. Epub 2014 Jan 14. Review. PubMed PMID: 24434059.
8: 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. doi: 10.1038/onc.2013.418. [Epub ahead of print] PubMed PMID: 24141786.
9: Davar D, Tarhini AA, Kirkwood JM. Adjuvant immunotherapy of melanoma and development of new approaches using the neoadjuvant approach. Clin Dermatol. 2013 May-Jun;31(3):237-50. doi: 10.1016/j.clindermatol.2012.08.012. Review. Erratum in: Clin Dermatol. 2013 Jul-Aug;31(4):501. PubMed PMID: 23608443; PubMed Central PMCID: PMC3654101.
10: Akinleye A, Furqan M, Mukhi N, Ravella P, Liu D. MEK and the inhibitors: from bench to bedside. J Hematol Oncol. 2013 Apr 12;6:27. doi: 10.1186/1756-8722-6-27. Review. PubMed PMID: 23587417; PubMed Central PMCID: PMC3626705.
CAS#: 606143-89-9
Chemical Formula: C17H15BrF2N4O3
Exact Mass: 440.02956
Molecular Weight: 441.22681
Elemental Analysis: C, 46.28; H, 3.43; Br, 18.11; F, 8.61; N, 12.70; O, 10.88
EOS Med Chem produce Binimetinib (MEK-162),606143-89-9 in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.
Binimetinib (MEK-162),606143-89-9 Intermediates, EOS Med Chem have 8; Binimetinib (MEK-162),606143-89-9 Impurity we have 10, all from GMP, FDA plant.
Now Binimetinib (MEK-162),606143-89-9 DMF document is preparing.
Until 2016, Aug, Binimetinib (MEK-162),606143-89-9 more than produced 25kg API, 120kg Intermediates
GMP PRODUCE:
Alectinib;Veliparib;Acalabrutinib;Venetoclax;Sotagliflozin;Ledipasvir;LX1606;Anacetrapib;Abemaciclib
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2016 Barcelona CPHI, Hope to meet!
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Binimetinib Binimetinib 606143-89-9
Binimetinib Intermediates MEK-162; ARRY-162; ARRY-438162; 606143-89-9
Binimetinib Intermediates Methyl 4-amino-2-((4-bromo-2-fluorophenyl)amino)-3-fluoro-5-nitrobenzoate
Binimetinib Intermediates Methyl 6-((4-bromo-2-fluorophenyl)amino)-7-fluoro-1H-benzo[d]imidazole-5-carboxylate 606143-48-0
Binimetinib Intermediates 5-((4-bromo-2-fluorophenyl)amino)-4-fluoro-1-methyl-1H-benzo[d]imidazole-6-carboxylic acid 1415564-99-6
Binimetinib Intermediates Methyl 5-((4-bromo-2-fluorophenyl)amino)-4-fluoro-1-methyl-1H-benzo[d]imidazole-6-carboxylate 1415559-93-1
Description: Binimetinib, also known as MEK162 (ARRY-162), is an oral, highly selective MEK inhibitor. In preclinical studies, MEK162 showed significant antitumor activities in cell lines and animal models. MEK162 is the first targeted therapy to show activity in patients with NRAS -mutated melanoma and might offer a new option for a cancer with few effective treatments.
Synonym: MEK162; MEK-162; MEK 162; ARRY162; ARRY-162; ARRY 162; ARRY438162, Binimetinib
IUPAC/Chemical Name: 5-((4-bromo-2-fluorophenyl)amino)-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-1H-benzo[d]imidazole-6-carboxamide.
SMILES Code: O=C(C1=C(NC2=CC=C(Br)C=C2F)C(F)=C3N=CN(C)C3=C1)NOCCO
1: Hamidi H, Lu M, Chau K, Anderson L, Fejzo M, Ginther C, Linnartz R, Zubel A, Slamon DJ, Finn RS. KRAS mutational subtype and copy number predict in vitro response of human pancreatic cancer cell lines to MEK inhibition. Br J Cancer. 2014 Aug 28. doi: 10.1038/bjc.2014.475. [Epub ahead of print] PubMed PMID: 25167228.
2: Rebecca VW, Alicea GM, Paraiso KH, Lawrence H, Gibney GT, Smalley KS. Vertical inhibition of the MAPK pathway enhances therapeutic responses in NRAS-mutant melanoma. Pigment Cell Melanoma Res. 2014 Aug 11. doi: 10.1111/pcmr.12303. [Epub ahead of print] PubMed PMID: 25130256.
3: 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 Jul;25(7):1437-41. doi: 10.1093/annonc/mdu169. Epub 2014 May 26. PubMed PMID: 24864047.
4: Küsters-Vandevelde HV, Willemsen AE, Groenen PJ, Küsters B, Lammens M, Wesseling P, Djafarihamedani M, Rijntjes J, Delye H, Willemsen MA, van Herpen CM, Blokx WA. Experimental treatment of NRAS-mutated neurocutaneous melanocytosis with MEK162, a MEK-inhibitor. Acta Neuropathol Commun. 2014 Apr 8;2(1):41. doi: 10.1186/2051-5960-2-41. PubMed PMID: 24713450; PubMed Central PMCID: PMC4023633.
5: 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. doi: 10.1186/1476-4598-13-45. PubMed PMID: 24588908; PubMed Central PMCID: PMC3945937.
6: Gritsman K, Yuzugullu H, Von T, Yan H, Clayton L, Fritsch C, Maira SM, Hollingworth G, Choi C, Khandan T, Paktinat M, Okabe RO, Roberts TM, Zhao JJ. Hematopoiesis and RAS-driven myeloid leukemia differentially require PI3K isoform p110α. J Clin Invest. 2014 Apr 1;124(4):1794-809. doi: 10.1172/JCI69927. Epub 2014 Feb 24. PubMed PMID: 24569456; PubMed Central PMCID: PMC3973083.
7: Miller CR, Oliver KE, Farley JH. MEK1/2 inhibitors in the treatment of gynecologic malignancies. Gynecol Oncol. 2014 Apr;133(1):128-37. doi: 10.1016/j.ygyno.2014.01.008. Epub 2014 Jan 14. Review. PubMed PMID: 24434059.
8: 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. doi: 10.1038/onc.2013.418. [Epub ahead of print] PubMed PMID: 24141786.
9: Davar D, Tarhini AA, Kirkwood JM. Adjuvant immunotherapy of melanoma and development of new approaches using the neoadjuvant approach. Clin Dermatol. 2013 May-Jun;31(3):237-50. doi: 10.1016/j.clindermatol.2012.08.012. Review. Erratum in: Clin Dermatol. 2013 Jul-Aug;31(4):501. PubMed PMID: 23608443; PubMed Central PMCID: PMC3654101.
10: Akinleye A, Furqan M, Mukhi N, Ravella P, Liu D. MEK and the inhibitors: from bench to bedside. J Hematol Oncol. 2013 Apr 12;6:27. doi: 10.1186/1756-8722-6-27. Review. PubMed PMID: 23587417; PubMed Central PMCID: PMC3626705.
