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Cobimetinib

Cobimetinib (GDC-0973) 是一种可口服的 MEK1选择性抑制剂，抑制MEK1的IC50为4.2 nM。

CAS号

934660-93-2

分子式

C21H21F3IN3O2

主要靶点

MEK|Apoptosis

仅限科研使用

Cat No : CM05060

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Synonyms

GDC-0973|考比替尼|RG7420|XL518|可美替尼

验证数据展示

  • CAS No.: 934660-93-2

    Cobimetinib
    CAS#: 934660-93-2

产品信息

Cobimetinib is a selective inhibitor of mitogen-activated protein kinase kinase (MEK) (IC50: 0.9 nM). Cobimetinib specifically binds to and inhibits the catalytic activity of MEK1, resulting in inhibition of extracellular signal-related kinase 2 (ERK2) phosphorylation and activation and decreased tumor cell proliferation.

CAS号 934660-93-2
分子式 C21H21F3IN3O2
主要靶点 MEK|Apoptosis
主要通路 MAPK信号通路|凋亡
分子量 531.32
纯度 100.00%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 GDC-0973|考比替尼|RG7420|XL518|可美替尼

靶点活性

MEK:0.9 nM

体内活性

Cobimetinib对多种肿瘤细胞生长均有强烈的抑制作用,尤其是KRAS或BRAF突变型癌细胞系。Cobimetinib与GDC-0941联用可降低888MEL和A2058细胞的生存能力,并抑制通路、增加细胞凋亡。[1]Cobimetinib和vemurafenib联用可使所有BRAFV600E系中细胞膜上的GLUT-1减少程度显著加剧。

体外活性

在负荷KRAS和BRAFV600E突变型肿瘤的小鼠体内,Cobimetinib (10 mg/kg, p.o.)对肿瘤病程有抑制作用.[1]在负荷耐药的A375异种移植物小鼠体内,Cobimetinib与GDC-0941联用还可减少己糖激酶II,Ksr,c-RAF 和p-MEK蛋白质的水平.

溶解度

Ethanol:44 mg/mL (82.8 mM),H2O:<1 mg/mL,DMSO:93 mg/mL (175 mM)

细胞实验

Cells are plated in quadruplicate at a density of 3,000 per well in 384-well plates in normal growth medium and allowed to adhere overnight. Compounds are added in 10 concentrations based on a 3-fold dilution series. Cell viability is measured 72 h later using the CellTiter-Glo Luminescent Cell Viability Assay.(Only for Reference)

参考文献

1.Hoeflich KP, et al. Cancer Res. 2012, 72(1), 210-219. 2.Baudy AR, et al. EJNMMI Res. 2012, 2(1), 22.

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
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