Cobimetinib (GDC-0973, RG7420)

目录号:S8041 别名: XL518

Cobimetinib (GDC-0973, RG7420) Chemical Structure

Molecular Weight(MW): 531.31

Cobimetinib (GDC-0973, RG7420)是一种有效的高选择性MEK1抑制剂,IC50 为 4.2 nM。其对MEK1的选择性比对MEK2高100倍以上,对其他很多丝氨酸-苏氨酸和酪氨酸激酶没有显著抑制作用。Phase 3。

规格 价格 库存 购买数量  
RMB 1631.78 现货
RMB 4889.23 现货
RMB 8174.33 现货
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客户使用Selleck该产品发表文献15篇:

客户使用该产品的3个实验数据:

  • Three types of selective inhibitors of MAPK signaling produce expected differential kinase inhibition and activation responses in HCT116 colorectal cancer cells. HCT116 cells were treated with 250 nM of GDC-0973, GDC-0623, SCH772984 or DMSO for 1, 4, or 24 h. In the washout samples, cells were drug treated for 24 h, then changed into fresh media and harvested after 0.5 or 2 h. Lysates were used for Western blots of total and phosphorylated MEK, ERK, and RSK; blotting for COX IV was used as the loading control.

    Mol Cell Proteomics, 2017, 16(2):265-277. Cobimetinib (GDC-0973, RG7420) purchased from Selleck.

  • Western blots showing protein changes of p21, p53, cyclin D1, and cyclin E in HCT116 cells after treatment with 1 μM cobimetinib over different timespans.

    Cell Physiol Biochem, 2018, 47(2):680-693. Cobimetinib (GDC-0973, RG7420) purchased from Selleck.

  • Human-washed platelet aggregation was performed by optical aggregometry following stimulation with U46619 (0.25μM) in the presence or absence of LPS from E. coli O111:B4 (1μg/mL) after 3 min of incubation with Cobimetinib (100μM) before activation with U46619 (0.25μM) (B).

    PLoS One, 2017, 12(11):e0186981. Cobimetinib (GDC-0973, RG7420) purchased from Selleck.

产品安全说明书

MEK抑制剂选择性比较

生物活性

产品描述 Cobimetinib (GDC-0973, RG7420)是一种有效的高选择性MEK1抑制剂,IC50 为 4.2 nM。其对MEK1的选择性比对MEK2高100倍以上,对其他很多丝氨酸-苏氨酸和酪氨酸激酶没有显著抑制作用。Phase 3。
靶点
MEK1 [1]
(Cell-free assay)
4.2 nM
体外研究

Cobimetinib对一组广泛类型的肿瘤细胞的生长表现出强烈的抑制活性,特别是对BRAF或KRAS突变型癌细胞系。结合GDC-0941,GDC-0973在888MEL和A2058细胞中导致生存能力降低,通路抑制,以及细胞凋亡增加。[1] GDC-0973和vemurafenib联合给药显著增加所有BRAFV600E系中细胞膜上减少的GLUT-1水平。[2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human MDA-MB-231T cells MmLzSpVv[3Srb36gZZN{[Xl? NWX5V45vOSCq NFHYe5hKdmirYnn0bY9vKG:oIF3FT{1u\WSrYYTl[EBGWktiVEKwNk9[OjB2IIDoc5NxcG:{eXzheIlwdiCrbjDoeY1idiCPRFGtUWIuOjNzVDDj[YxteyCjZoTldkAyKGi{IHL5JIludXWwb3Lsc5R1cW6p78{MJGlEPTB;MD6yJI5O M2K3cFI1QTByNEi2
human COLO205 cells NFW2RnRHfW6ldHnvckBie3OjeR?= NWrneXQzUW6qaXLpeIlwdiCxZjDCMZJi\iCYNkCwSUBufXSjboSgbY4hcHWvYX6gR29NVzJyNTDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gc4YhTVKNMT;FVmszKHCqb4PwbI9zgWyjdHnvckwhUUN3ME2xMlghdk1? NY[wV2NrOjJ|MUWzN|I>
human COLO205 cells NInBWoNRem:uaX\ldoF1cW:wIHHzd4F6 NYq4eox6SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDDU2xQOjB3IHPlcIx{KGW6cILld5NqdmdiQj3yZYYhXjZyMFWgcZV1[W62LDDJR|UxRThibl2= M3frVFIzOzF3M{Oy

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
pERK / ERK / MCL-1 / p-MCL1 / BIM / cleaved PARP; 

PubMed: 27765849     


RKO cells were treated with increasing doses of cobimetinib for 48 h and protein expression, including BIM isoforms [extra long (EL), long (L) and short (S)] and PARP cleavage (CL), were analyzed by immunboblotting. 

p-c-RAF / c-RAF / p-MEK / MEK; 

PubMed: 26384788     


Effect of cobimetinib on MAPK cascade pathway. Changes in activation status of RAF, MEK and ERK were evaluated in three NB cell lines after treatment with cobimetinib (1 μM) or DMSO for four hours. Cell lysates were made with lysis buffer containing prote䲧疝Ỵ疞㧀疜膉痘 瘿⟸෕ᾰƌ෕Ð 㺣痖帉痖Ѐ瑖堘𢡄빢᎒෕Ð鑸᎒彿堙奋堙巫堙᎒ﻺ᎒彿堙ﻮ᎒塚堙ﻺ᎒ꍈ堞빢᎒學堙漸堞圔堙빢᎒圞堙圭堙𢡄玚Wᾰƌ ᾰƌ戤瘯Ɖ�෋䐺痖暼瘿�෋ᾰƌ �෋Ð㺣痖�෋

27765849 26384788
Growth inhibition assay
Cell viability ; 

PubMed: 28098866     


MEL-XY3 cells were treated with different concentrations of GDC-0973 (0–10 µM) for 72 h and viability was determined using MTT assay. 

28098866
体内研究 在负荷BRAFV600E和KRAS突变型肿瘤的小鼠体内,Cobimetinib (10 mg/kg, p.o.)产生抗肿瘤作用,结合GDC-0973和GDC-0941能够提高疗效。[1]在负荷耐药的A375异种移植物小鼠体内,GDC-0973与GDC-0941结合诱导己糖激酶II,c-RAF,Ksr 和p-MEK蛋白质的水平减少。[2]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

动物实验:

[1]

+ 展开
  • Animal Models: 负荷Molm-13,Molm-16,MX-1,DLD-1,HCT-116,LoVo,FaDu,537MEL,A2058,A2058-X1,A375,A375.X1,A427,A549,Calu-6,EBC-1,NCI-H441,NCI-H2122,NCI-H460,NCI-H520.X1,SKOV-3,KP4-X1.1,MiaPaCa-2,22Rv1,DU-145.X1,S,NCI-H69 异种移植瘤的小鼠
  • Formulation: --
  • Dosages: 10 mg/kg
  • Administration: p.o.
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 100 mg/mL (188.21 mM)
Ethanol 47 mg/mL warmed (88.46 mM)
Water Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
5% DMSO+30% PEG 300+5% Tween 80+ddH2O
5mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 531.31
化学式

C21H21F3IN3O2

CAS号 934660-93-2
储存条件 powder
in solvent
别名 XL518

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03732703 Not yet recruiting Relapsed Refractory Multiple Myeloma Multiple Myeloma Research Consortium|AbbVie|Celgene Corporation|Eli Lilly and Company|Genentech Inc.|Janssen LP|Takeda March 15 2019 Phase 1|Phase 2
NCT03732703 Not yet recruiting Relapsed Refractory Multiple Myeloma Multiple Myeloma Research Consortium|AbbVie|Celgene Corporation|Eli Lilly and Company|Genentech Inc.|Janssen LP|Takeda March 15 2019 Phase 1|Phase 2
NCT03625141 Recruiting Metastatic Melanoma Hoffmann-La Roche December 13 2018 Phase 2
NCT03625141 Recruiting Metastatic Melanoma Hoffmann-La Roche December 13 2018 Phase 2
NCT03695380 Recruiting OVARIAN CANCER Hoffmann-La Roche November 2 2018 Phase 1
NCT03695380 Recruiting OVARIAN CANCER Hoffmann-La Roche November 2 2018 Phase 1

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操作手册

如果有其他问题,请给我们留言。

  • * 必填项

常见问题及建议解决方法

  • 问题 1:

    How to reconstitute the inhibitor for in vivo studies?

  • 回答:

    S8041 can be dissolved in 5% DMSO/30% PEG 300/5% Tween 80/ddH2O at 5 mg/ml clearly and it is ok for both oral gavage and injection.

MEK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID