606143-89-9|Binimetinib (MEK-162)|5-((4-bromo-2-fluorophenyl)amino)-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-1H-benzo[d]imidazole-6-carboxamide.|-范德生物科技公司

Binimetinib (MEK-162)

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names：
5-((4-bromo-2-fluorophenyl)amino)-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-1H-benzo[d]imidazole-6-carboxamide.
CAS号：
606143-89-9
MDL Number：
MF(分子式)： C17H15BrF2N4O3 MW(分子量)： 441.22681
EINECS: Reaxys Number:
Pubchem ID: Brand:BIOFOUNT

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中文别名	Binimetinib (MEK-162)
英文别名	MEK162; MEK-162; MEK 162; ARRY162; ARRY-162; ARRY 162; ARRY438162, Binimetinib; Brand name Mektovi.
CAS号	606143-89-9
Inchi	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
分子式 Formula	C17H15BrF2N4O3
分子量 Molecular Weight	441.22681
溶解度Solubility
性状	Solid powder
储藏条件 Storage conditions	Dry, dark and store at 0-4℃ for short term (days to weeks) or -20℃ for long term (Store correctly 2-3years).

产品说明	Binimetinib (MEK-162)(CAS:606143-89-9):仅限应用于工业或者科学研究过程中非医疗目的，不应用于人类或动物的临床诊断以及治过程疗，该产品非药用，非食用。
Introduction	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.
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[1]McLoughlin EM, Fadul CE, Patel SH, Hall RD, Gentzler RD. Clinical and Radiographic Response of Leptomeningeal and Brain Metastases to Encorafenib and Binimetinib in a Patient With BRAF V600E-Mutated Lung Adenocarcinoma. J Thorac Oncol. 2019 Dec;14(12):e269-e27[1]doi: 10.1016/j.jtho.2019.07.019. PubMed PMID: 31757377.

[2]Gravbrot N, Sundararajan S. Severe Drug-Induced Liver Injury from Combination Encorafenib/Binimetinib. Case Rep Oncol Med. 2019 Oct 7;2019:3051945. doi: 10.1155/2019/3051945. eCollection 2019. PubMed PMID: 31687241; PubMed Central PMCID: PMC6800898.

[3] Holbrook K, Lutzky J, Davies MA, Davis JM, Glitza IC, Amaria RN, Diab A, Patel SP, Amin A, Tawbi H. Intracranial antitumor activity with encorafenib plus binimetinib in patients with melanoma brain metastases: A case series. Cancer. 2019 Oct 28. doi: 10.1002/cncr.32547. [Epub ahead of print] PubMed PMID: 31658370.

[4] Binimetinib plus encorafenib for metastatic melanoma. Aust Prescr. 2019 Oct;42(5):168. doi: 10.18773/austprescr.2019.057. Epub 2019 Sep 13. Review. PubMed PMID: 31631932; PubMed Central PMCID: PMC6787304.

[5] Kopetz S, Grothey A, Yaeger R, Van Cutsem E, Desai J, Yoshino T, Wasan H, Ciardiello F, Loupakis F, Hong YS, Steeghs N, Guren TK, Arkenau HT, Garcia-Alfonso P, Pfeiffer P, Orlov S, Lonardi S, Elez E, Kim TW, Schellens JHM, Guo C, Krishnan A, Dekervel J, Morris V, Calvo Ferrandiz A, Tarpgaard LS, Braun M, Gollerkeri A, Keir C, Maharry K, Pickard M, Christy-Bittel J, Anderson L, Sandor V, Tabernero J. Encorafenib, Binimetinib, and Cetuximab in BRAF V600E-Mutated Colorectal Cancer. N Engl J Med. 2019 Oct 24;381(17):1632-1643. doi: 10.1056/NEJMoa1908075. Epub 2019 Sep 30. PubMed PMID: 31566309.

6: Ngo P, Bycroft R. Encorafenib and binimetinib for the treatment of BRAF-mutated metastatic melanoma in the setting of combined hepatic and renal impairment. BMJ Case Rep. 2019 Sep 16;12(9). pii: e230974. doi: 10.1136/bcr-2019-230974. PubMed PMID: 31527213.7: Gogas HJ, Flaherty KT, Dummer R, Ascierto PA, Arance A, Mandala M, Liszkay G, Garbe C, Schadendorf D, Krajsova I, Gutzmer R, Sileni VC, Dutriaux C, de Groot JWB, Yamazaki N, Loquai C, Gollerkeri A, Pickard MD, Robert C. Adverse events associated with encorafenib plus binimetinib in the COLUMBUS study: incidence, course and management. Eur J Cancer. 2019 Sep;119:97-106. doi: 10.1016/j.ejca.2019.07.016. Epub 2019 Aug 19. PubMed PMID: 31437754.8: Goldinger SM, Valeska Matter A, Urner-Bloch U, Narainsing J, Micaletto S, Blume I, Mangana J, Dummer R. Binimetinib in heavily pretreated patients with NRAS-mutant melanoma with brain metastases. Br J Dermatol. 2019 Aug 22. doi: 10.1111/bjd.18449. [Epub ahead of print] PubMed PMID: 31436845.9: Bardia A, Gounder M, Rodon J, Janku F, Lolkema MP, Stephenson JJ, Bedard PL, Schuler M, Sessa C, LoRusso P, Thomas M, Maacke H, Evans H, Sun Y, Tan DSW. Phase Ib Study of Combination Therapy with MEK Inhibitor Binimetinib and Phosphatidylinositol 3-Kinase Inhibitor Buparlisib in Patients with Advanced Solid Tumors with RAS/RAF Alterations. Oncologist. 2019 Aug 8. pii: theoncologist.2019-0297. doi: 10.1634/theoncologist.2019-0297. [Epub ahead of print] PubMed PMID: 31395751.10: Kim JW, Lee KH, Kim JW, Suh KJ, Nam AR, Bang JH, Bang YJ, Oh DY. Enhanced antitumor effect of binimetinib in combination with capecitabine for biliary tract cancer patients with mutations in the RAS/RAF/MEK/ERK pathway: phase Ib study. Br J Cancer. 2019 Aug;121(4):332-339. doi: 10.1038/s41416-019-0523-5. Epub 2019 Jul 17. PubMed PMID: 31312030; PubMed Central PMCID: PMC6738070.1

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