AZ 628

目录号:S2746

仅限科研使用

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。

AZ 628 Chemical Structure

CAS: 878739-06-1

规格 价格 库存 购买数量
RMB 1225.39 现货
RMB 3841.45 现货
大包装 有超大折扣

今日订购,明日送达 全国免运费 分装免费 分装成小规格产品(单支最小为1mg)
如1支10mg产品可分装为10支1mg产品

全国免费电话:400-668-6834   |   Email:info@selleck.cn

客户使用Selleck生产的AZ 628发表文献38篇:

产品安全说明书

Raf抑制剂选择性比较

相关Raf产品

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 M{m1WGZ2dmO2aX;uJIF{e2G7 M17Pe|IxKG2rboO= MonDTY5pcWKrdHnvckBw\iCqdX3hckBz\WOxbXLpcoFvfCCQLYTldo1qdnW|IFjpd{11[WepZXSgRnJCTiCYNkCwSUBufXSjboSg[ZhxemW|c3XkJIlvKFOoOTDj[YxteyClb3X4dJJme3OrbnegR2REOzdidYPpcoch[mmxdHnufYxifGWmIF3FT{BieyC|dXLzeJJifGViYX7kJG1oS2x{IHnuZ5Vj[XSnZDDmc5IhOjBibXnud{BxemmxcjD0c{BO\0OuMjDh[IRqfGmxbjDt[YF{fXKnZDDh[pRmeiBzIHjyJIlvKHC{ZYPlcoNmKG:oIEGwJJVOKEGWUDygTWM2OD1yLkCzOO69VQ>? NVLSRXM2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOzPVg1PTNpPkKzN|k5PDV|PD;hQi=>
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Sf9 M3TPUmZ2dmO2aX;uJIF{e2G7 NIjST4wzOCCvaX7z NHPaVnNKdmirYnn0bY9vKG:oIHj1cYFvKHKnY3;tZolv[W62IF6teIVzdWmwdYOgTIl{NXSjZ3fl[EBDWkGIIHX4dJJme3OnZDDpckBU\jliY3XscJMh[2:neIDy[ZN{cW6pIFPER|M4KHW|aX7nJIJqd3SrbonsZZRm\CCPRVugZZMhe3Wkc4TyZZRmKGGwZDDN[2NtOiCrbnP1ZoF1\WRiZn;yJFIxKG2rboOgdJJqd3JidH:gUYdEdDJiYXTkbZRqd25ibXXhd5Vz\WRiYX\0[ZIhOSCqcjDpckBxemW|ZX7j[UBw\iB3IH3NJGFVWCxiSVO1NF0zNjZ2zszN M1[wc|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|M{m4OFU{Lz5{M{O5PFQ2OzxxYU6=
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MCF7 NEH0ToJHfW6ldHnvckBie3OjeR?= M3u3UFc2KG2rboO= M4nOeGlvcGmkaYTpc44hd2Zid3ns[EB1gXCnIFLSRWYhcW5iaIXtZY4hVUOINzDj[YxteyCjc4Pld5Nm\CCjczDk[YNz\WG|ZTDpckBGWkticHjvd5Bpd3K7bHH0bY9vKGGodHXyJFc2KG2rboOgZpkhX2W|dHXyckBjdG:2dHnu[{BidmGueYPpdy=> Mo\tQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN|OUi0OVMoRjJ|M{m4OFU{RC:jPh?=
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SKBR3 MYfBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NHfk[YQ4OiCqcoO= MkK2RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVS1LSN{Bk\WyuczDlfJBz\XO|aX7nJJdqdGRidInw[UBDWkGIIHHmeIVzKDd{IHjyd{BjgSCPVGOgZZN{[Xl? MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzN7OES1N{c,OjN|OUi0OVM9N2F-
MCF7 NFH0VppCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= M4\5flczKGi{cx?= Mnq5RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPQ1[3JINmdGy|IHX4dJJme3Orbnege4lt\CC2eYDlJGJTSUZiYX\0[ZIhPzJiaILzJIJ6KE2WUzDhd5NigQ>? NF3sVYU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{O5PFQ2Oyd-MkOzPVg1PTN:L3G+
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OCUB-M MYPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVLJcohq[mm2aX;uJI9nKGi3bXHuJG9EXUJvTTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUS2MlkzPDoQvF2= NVzlcXkzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjF2NEC2PU8oRlODTlfFVlww[T5?
TGW Mo\HS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXLqTnU4UW6qaXLpeIlwdiCxZjDoeY1idiCWR2egZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20O{43OjJ{zszN Mo\EQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlE1PDB4OT:nQnNCVkeHUkyvZV4>
OS-RC-2 MWfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MYHJcohq[mm2aX;uJI9nKGi3bXHuJG9UNVKFLUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20PE4xOzh7zszN NFXZ[pI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTR2ME[5M{c,W0GQR1XSQE9iRg>?
D-542MG M{O1dmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M1nWWmlvcGmkaYTpc44hd2ZiaIXtZY4hTC13NELNS{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQ6NjZ2NkpOwG0> MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVQ1ODZ7Lze+V2FPT0WUPD;hQi=>
Assay
Methods Test Index PMID
Western blot p-ERK / ERK / p-MEK / MEK / BIM / BRAF / CRAF 21098728
Growth inhibition assay Cell viability 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]
  • 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。

溶解度(25°C)

体外

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 3年 -20°C 粉状
2年 -80°C 溶于溶剂

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)

mg/kg g μL

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
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

摩尔浓度计算器

质量 浓度 体积 分子量

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

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