Hot Line:137-9521-9287

Binimetinib

Time:2016-10-31

Binimetinib

CAS#: 606143-89-9

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.

THEORETICAL ANALYSIS

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

TECHNICAL DATA

Appearance:
Solid powder
Purity:
>98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition:
Dry, dark and at 0 – 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility:
Soluble in DMSO, not in water
Shelf Life:
>2 years if stored properly
Drug Formulation:
This drug may be formulated in DMSO
Stock Solution Storage:
0 – 4 C for short term (days to weeks), or -20 C for long term (months).

REFERENCES

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.

Previous: Next: