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Binimetinib

MEK 162,MEK-162,MEK162,ARRY 162,ARRY162,ARRY-162,ARRY 438162

MEK162(ARRY-438162; ARRY-162)是MEK1/2抑制剂，IC50为12 nM。

目录号
EY1377
EY1377
EY1377
EY1377
纯度
99.45%
99.45%
99.45%
99.45%
规格
5 mg
10 mg
50 mg
100 mg
原价
420
660
1800
2700
售价
420
660
1800
2700
库存
现货
现货
现货
现货
订购
订购
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  • 生物活性

    Binimetinib (MEK162, ARRY-162, ARRY-438162) is a potent inhibitor of MEK1/2 with IC50 of 12 nM in a cell-free assay. Phase 3.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

  • 动物实验

    6 mg/kg 口服处理

  • 不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

    动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数


    例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。

  • 参考文献

    [1] J Pheneger, et al. 2006, ACR Annual Scientific Meeting. Abst 794.

    分子式
    C17H15BrF2N4O3    		 分子量
    441.23    		 CAS号
    606143-89-9    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    85 mg/mL    		 Water
    <1 mg/mL    		 Ethanol
    <1 mg/mL

    体内溶解度

  • Clinical Trial Information ( data from http://clinicaltrials.gov )

    NCT Number Conditions Interventions Sponsor/Collaborators Phases Start Date Last Updated
    NCT02964689 Advanced Non-small Cell Lung Cancer|KRAS Gene Mutation|Lung Cancer Drug: Binimetinib|Drug: Pemetrexed|Drug: Cisplatin Swiss Group for Clinical Cancer Research Phase 1 2017-03-01 2016-11-14
    NCT02185690 Lungcancer Drug: Binimetinib|Drug: Pemetrexed|Drug: Carboplatin University Health Network, Toronto|Novartis Pharmaceuticals Phase 1 2017-03-01 2016-12-05
    NCT02451865 Recurrent Non-Small Cell Lung Carcinoma|Stage IV Non-Small Cell Lung Cancer Drug: Binimetinib|Drug: Docetaxel|Other: Laboratory Biomarker Analysis Jonsson Comprehensive Cancer Center|National Cancer Institute (NCI) Phase 1 2016-06-01 2016-07-07
    NCT02613650 Advanced KRAS Positive Metastatic Colorectal Cancer Drug: MEK162 and mFOLFIRI University of Utah|Array BioPharma Phase 1 2016-05-12 2017-02-15
    NCT02050815 Hepatic Impairment Drug: MEK162 Array BioPharma Phase 1 2014-03-01 2017-03-09
    NCT01885195 Solid Tumor and Hematologic Malignancies Drug: MEK162 Array BioPharma Phase 2 2013-10-01 2017-03-01
    NCT02773459 Biliary Tract Cancer Drug: MEK162+capecitabine Seoul National University Hospital Phase 1|Phase 2 2016-04-01 2016-05-15
    NCT01562899 Metastatic Pancreatic Adenocarcinoma|BRAF Mutated Melanoma Drug: MEK162|Drug: AMG 479 Array BioPharma Phase 2 2012-08-01 2017-02-14
    NCT01469130 Advanced Solid Tumor Drug: MEK162 Array BioPharma Phase 1 2011-11-01 2017-02-17
    NCT01449058 Advanced and Selected Solid Tumors, AML, High Risk and Very High Risk MDS Drug: BYL719 plus MEK162 Array BioPharma Phase 1|Phase 2 2012-03-01 2017-02-17
    NCT02089230 Leukemia Drug: MEK 162 M.D. Anderson Cancer Center|Array BioPharma Phase 1|Phase 2 2014-08-01 2016-11-29
    NCT01828034 Advanced Biliary Tract Carcinoma Drug: Gemcitabine|Drug: Cisplatin|Drug: MEK162 Memorial Sloan Kettering Cancer Center|Array BioPharma Phase 1|Phase 2 2013-04-01 2016-12-19
    NCT02263898 Recurrent Melanoma|Stage IV Melanoma Drug: Raf kinase inhibitor LGX818|Drug: binimetinib|Other: laboratory biomarker analysis Jonsson Comprehensive Cancer Center|National Cancer Institute (NCI) Phase 2 2015-01-01 2016-12-20
    NCT01556568 Cardiomegaly Drug: MEK162 Array BioPharma Phase 2 2012-02-01 2015-12-28
    NCT02285439 Low-Grade Gliomas|Malignant Neoplasms, Brain|Soft Tissue Neoplasms Drug: MEK162 Children's Hospital Los Angeles|Dana-Farber Cancer Institute Phase 1|Phase 2 2016-04-01 2017-01-23
    NCT02834364 Relapsed or Refractory Multiple Myeloma|Patients With BRAFV600 E or BRAFV600K Mutation Drug: Encorafenib|Drug: Binimetinib University of Heidelberg Medical Center|Array BioPharma|German Cancer Research Center|Coordinating Centre for Clinical Trials Heidelberg|University Hospital Heidelberg Phase 2 2016-06-01 2016-07-12
    NCT02049801 Adult Acute Minimally Differentiated Myeloid Leukemia (M0)|Adult Acute Monoblastic Leukemia (M5a)|Adult Acute Monocytic Leukemia (M5b)|Adult Acute Myeloblastic Leukemia With Maturation (M2)|Adult Acute Myeloblastic Leukemia Without Maturation (M1)|Adult Acute Myeloid Leukemia With 11q23 (MLL) Abnormalities|Adult Acute Myeloid Leukemia With Del(5q)|Adult Acute Myeloid Leukemia With Inv(16)(p13;q22)|Adult Acute Myeloid Leukemia With t(15;17)(q22;q12)|Adult Acute Myeloid Leukemia With t(16;16)(p13;q22)|Adult Acute Myeloid Leukemia With t(8;21)(q22;q22)|Adult Acute Myelomonocytic Leukemia (M4)|Adult Erythroleukemia (M6a)|Adult Pure Erythroid Leukemia (M6b)|Recurrent Adult Acute Myeloid Leukemia Drug: MEK inhibitor MEK162|Drug: idarubicin|Drug: cytarabine|Other: pharmacological study|Other: laboratory biomarker analysis Bruno C. Medeiros|National Cancer Institute (NCI)|Stanford University Phase 1 2014-12-01 2017-01-26
    NCT01801358 Uveal Melanoma Drug: AEB071|Drug: MEK162 Array BioPharma Phase 1|Phase 2 2013-08-01 2016-08-29
    NCT02225574 Leukemia Drug: MEK-162|Drug: Nilotinib|Behavioral: Questionnaires M.D. Anderson Cancer Center|Array BioPharma Phase 1|Phase 2 2015-03-11 2017-02-03
    NCT02902042 Malignant Melanoma Drug: Encorafenib|Drug: Binimetinib|Drug: Pembrolizumab|Drug: Pembrolizumab alone Prof. Dr. med. Dirk Schadendorf|University Hospital, Essen Phase 1|Phase 2 2016-12-01 2016-09-16
    NCT02041481 Recurrent Colon Cancer|Recurrent Rectal Cancer|Stage IVA Colon Cancer|Stage IVA Rectal Cancer|Stage IVB Colon Cancer|Stage IVB Rectal Cancer Drug: MEK inhibitor MEK162|Drug: leucovorin calcium|Drug: fluorouracil|Drug: oxaliplatin|Other: pharmacological study|Other: Laboratory Biomarker Analysis City of Hope Medical Center|National Cancer Institute (NCI)|Array BioPharma Phase 1 2014-06-01 2016-09-02
    NCT01991379 Gastrointestinal Stromal Tumor (GIST) Drug: MEK162|Drug: Imatinib Mesylate (Gleevec; STI571; NSC #716051)|Other: Blood draws|Procedure: biopsy Memorial Sloan Kettering Cancer Center|Array BioPharma|University of Pittsburgh Phase 1|Phase 2 2013-11-01 2016-08-31
    NCT01337765 Unspecified Adult Solid Tumor, Protocol Specific|Solid Tumor Drug: BEZ235 + MEK162 Array BioPharma Phase 1 2011-07-01 2016-02-11
    NCT01320085 BRAF or NRAS Mutant Metastatic Melanoma Drug: MEK162 Array BioPharma Phase 2 2011-03-01 2017-01-31
    NCT02105350 Biliary Tract Carcinoma|Gallbladder Carcinoma Drug: MEK 162|Drug: Gemcitabine|Drug: Oxaliplatin University Health Network, Toronto Phase 1 2015-06-01 2015-07-06

    注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。

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