AZ 628

For research use only. Not for use in humans.

目录号:S2746

AZ 628 Chemical Structure

CAS No. 878739-06-1

AZ628 是一种新型泛Raf抑制剂,作用于BRAF,BRAFV600E和c-Raf-1,无细胞试验中IC50分别为105 nM,34 nM和29 nM,也抑制VEGFR2, DDR2, Lyn, Flt1, FMS等。AZ628 可诱导凋亡。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 2191.76 现货
RMB 1225.39 现货
RMB 3841.45 现货
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客户使用Selleck生产的AZ 628发表文献34篇:

产品安全说明书

Raf抑制剂选择性比较

生物活性

产品描述 AZ628 是一种新型泛Raf抑制剂,作用于BRAF,BRAFV600E和c-Raf-1,无细胞试验中IC50分别为105 nM,34 nM和29 nM,也抑制VEGFR2, DDR2, Lyn, Flt1, FMS等。AZ628 可诱导凋亡。
靶点
C-Raf-1 [1]
(Cell-free assay)
B-Raf (V600E) [1]
(Cell-free assay)
B-Raf [1]
(Cell-free assay)
29 nM 34 nM 105 nM
体外研究

AZ628抑制B-Raf,B-RafV600E和c-Raf-1活性,IC50值分别为105,34和29 nM。AZ628也抑制多种酪氨酸蛋白激酶包括VEGFR2, DDR2, Lyn, Flt1, FMS等的激活。[1] AZ628作用于含B-RafV600E突变的结肠和恶性黑色素瘤细胞系,抑制锚蛋白依赖和非依赖性的生长, 引起细胞周期停滞,且诱导细胞凋亡。AZ628交叉反应谱说明AZ628和sorafenib相似,可以抗血管生成。[1] 用浓度不断升高的AZ628处理M14亲本细胞系,可观察到有效抑制p-ERK1/2水平。 抗AZ628的克隆表达CRAF提高。[2]提高的CRAF表达是抗连续AZ628处理的一种潜在机制,导致ERK1/2的持久激活。在对AZ628不敏感的细胞系中有三分之一用AZ628处理,不会明显抑制p-ERK1/2活性。AZ628作用于抗AZ628的M14细胞,不会抑制ERK的激活, AZ628作用于NRAS突变的恶性黑色素瘤细胞,有效降低ERK激活。[2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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Sf9 M3zmSWZ2dmO2aX;uJIF{e2G7 MU[yNEBucW6| MYDJcohq[mm2aX;uJI9nKGi3bXHuJJJm[2:vYnnuZY51KE5vdHXycYlvfXNiSHnzMZRi\2enZDDCVmFHKFZ4MEDFJI12fGGwdDDlfJBz\XO|ZXSgbY4hW2Z7IHPlcIx{KGOxZYjwdoV{e2mwZzDDSGM{PyC3c3nu[{BjcW:2aX75cIF1\WRiTVXLJIF{KHO3YoP0doF1\SCjbnSgUYdEdDJiaX7jeYJifGWmIH\vdkAzOCCvaX7zJJBzcW:{IITvJG1oS2x{IHHk[Il1cW:wIH3lZZN2emWmIHHmeIVzKDFiaIKgbY4heHKnc3XuZ4Uhd2ZiMUCgeW0hSVSSLDDJR|UxRTBwMEO0{txO NV\xNXh{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOzPVg1PTNpPkKzN|k5PDV|PD;hQi=>
Sf9 M4DYUGZ2dmO2aX;uJIF{e2G7 MoP5NlAhdWmwcx?= NYDRUnpUUW6qaXLpeIlwdiCxZjDoeY1idiC{ZXPvcYJqdmGwdDDOMZRmem2rboXzJGhqey22YXfn[YQhSlKDRjDWOlAxTSCvdYThcpQh\XiycnXzd4VlKGmwIGPmPUBk\WyuczDjc4V5eHKnc4PpcochS0SFM{egeZNqdmdiYnnveIlvgWyjdHXkJG1GUyCjczDzeYJ{fHKjdHWgZY5lKE2pQ3yyJIlv[3WkYYTl[EBnd3JiMkCgcYlveyCycnnvdkB1dyCPZ1PsNkBi\GSrdHnvckBu\WG|dYLl[EBi\nSncjCxJIhzKGmwIIDy[ZNmdmOnIH;mJFUhdU1iQWTQMEBKSzVyPUCuNlfPxE1? MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzN7OES1N{c,OjN|OUi0OVM9N2F-
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MCF7 M3XRUGZ2dmO2aX;uJIF{e2G7 NESwXII4PSCvaX7z M322ZmlvcGmkaYTpc44hd2Zid3ns[EB1gXCnIFLSRWYhcW5iaIXtZY4hVUOINzDj[YxteyCjc4Pld5Nm\CCjczDk[YNz\WG|ZTDpckBGWkticHjvd5Bpd3K7bHH0bY9vKGGodHXyJFc2KG2rboOgZpkhX2W|dHXyckBjdG:2dHnu[{BidmGueYPpdy=> MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzN7OES1N{c,OjN|OUi0OVM9N2F-
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OCUB-M MV;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MoToTY5pcWKrdHnvckBw\iCqdX3hckBQS1WELV2gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20Ok46OjR7zszN MkTQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlE1PDB4OT:nQnNCVkeHUkyvZV4>
TGW MWnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVfJcohq[mm2aX;uJI9nKGi3bXHuJHRIXyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTR5Lk[yNlLPxE1? NF3scVc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTR2ME[5M{c,W0GQR1XSQE9iRg>?
OS-RC-2 NI\VV2dIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mn;HTY5pcWKrdHnvckBw\iCqdX3hckBQWy2UQz2yJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OFgvODN6Od88US=> M3XKcVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyPDRyNkmvK|5USU6JRWK8M4E,
D-542MG M4rZPGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVO4cG06UW6qaXLpeIlwdiCxZjDoeY1idiCGLUW0Nm1IKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PDlwNkS2Pe69VQ>? MkKyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlE1PDB4OT:nQnNCVkeHUkyvZV4>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-ERK / ERK / p-MEK / MEK / BIM / BRAF / CRAF ; 

PubMed: 21098728     


Western blots of RAF-MEK pathway components and effectors in parental and AR cells treated with the indicated concentrations of AZ628 for 24 hours.

21098728
Growth inhibition assay
Cell viability ; 

PubMed: 21098728     


Parental (solid lines) COLO201 and COLO206F cells and AR (dashed lines) COLO201-AR and COLO206F-AR cells were treated in triplicate with the indicated concentrations of drug for 72 hours. Viable cell titer was determined, and the average values are shown relative to untreated controls for each cell line. Error bars represent the SD for each measurement. For each cell line, the IC50s for each inhibitor are shown in tabular form along with the increase in IC50 in AR cells relative to parental cells.

21098728

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)

细胞实验:[1]
- 合并
  • Cell lines: 表达BRAFV600E突变的M14细胞
  • Concentrations: 0.01-10 μM
  • Incubation Time: 过夜
  • Method: 0.5-2.5×105个M14细胞接种在12或24孔板上,板上有含5% FBS的培养基。 温育过夜后细胞用不同浓度AZ628处理。每两天更换新鲜培养基和药物,直到对照组每孔融合一起。移除培养基,细胞和溶于PBS的4%甲醛在室温下混合20分钟。然后用PBS冲洗细胞两次,用1:5000荧光核酸染料Syto60溶液染色。使用Odyssey红外成像仪在700 nm处测量荧光信号密度。每组实验重复进行四次,结果为四次结果的平均值。
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 90 mg/mL (199.32 mM)
Water Insoluble
Ethanol 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):
2% DMSO+40% PEG 300+2% Tween 80+ddH2O
6mg/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 451.52
化学式

C27H25N5O2

CAS号 878739-06-1
储存条件 粉状
溶于溶剂
别名 N/A

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

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 (mg) = 浓度 (mM) x 体积 (mL) 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、SDS / 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、SDS / 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

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题,请给我们留言。

  • * 必填项

Raf Signaling Pathway Map

Raf Inhibitors with Unique Features

相关Raf产品

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID