Ro-3306

目录号:S7747

仅限科研使用

RO-3306是一种ATP竞争性的选择性 CDK1 抑制剂,Ki 为20 nM,选择性是其他各种人类激酶的15倍多。RO-3306可增强p53介导的 Bax 激活和线粒体的凋亡。

Ro-3306 Chemical Structure

CAS: 872573-93-8

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 1138.82 现货
RMB 1049.39 现货
RMB 3270.12 现货
RMB 8151.52 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Ro-3306发表文献93篇:

产品安全说明书

CDK抑制剂选择性比较

相关CDK产品

生物活性

产品描述 RO-3306是一种ATP竞争性的选择性 CDK1 抑制剂,Ki 为20 nM,选择性是其他各种人类激酶的15倍多。RO-3306可增强p53介导的 Bax 激活和线粒体的凋亡。
靶点
CDK1 [1]
(Cell-free assay)
PKCδ [1]
(Cell-free assay)
SGK [1]
(Cell-free assay)
ERK [1]
(Cell-free assay)
20 nM(Ki) 318 nM(Ki) 497 nM(Ki) 1980 nM(Ki)
体外研究

RO-3306抑制CDK1/cyclin B1,CDK1/cyclin A,CDK2/cyclin E,和CDK4/cyclin D活性,Ki分别为35 nM,110 nM,340 nM,和>2000 nM。HCT116,SW480,和HeLa细胞用RO-3306处理20小时导致细胞周期完全阻滞在G2/M期。HCT116和SW480的增殖被RO-3306有效阻断。RO-3306似乎在癌细胞(HCT116和SW480)中比在非致瘤性细胞(MCF 10A和MCF 12A)中具有更强的促凋亡作用。[1] 10 μM 浓度的RO-3306有效阻止卵母细胞成熟。[2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
KB-3-1 adenocarcinoma cell line MoDBdWhVWyCjc4PhfS=> MWfQMYdtgWOxcILveIVqdiC|dXLzeJJifGW|IHnk[Y51cW[rZXSgbY4hU0JvMz2xJIFl\W6xY3HyZ4lvd22jIHPlcIwhdGmwZTygdWhVWyC2aHXyZZBmfXSrYzDsbYJz[XK7IIPjdoVmdg>? M2PWNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNzNUG1Nlg1Lz5|MUWxOVI5PDxxYU6=
human H460a cells M1TBTXBzd2yrZnXyZZRqd25iYYPzZZk> M3rJW2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSES2NIEh[2WubIOsJGlEPTB;MT6wOEDPxE1? MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzNyM{SyNUc,OTd|MEO0NlE9N2F-
human MDA435 cells Ml;6VJJwdGmoZYLheIlwdiCjc4PhfS=> MV\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2GQUSzOUBk\WyuczygTWM2OD1zLkG0JO69VQ>? NGrtb5c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{OwN|QzOSd-MUezNFM1OjF:L3G+
human HCT116 cells NHLodlRRem:uaX\ldoF1cW:wIHHzd4F6 MmraRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKQ2SxNVYh[2WubIOsJGlEPTB;MT6xOEDPxE1? MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzNyM{SyNUc,OTd|MEO0NlE9N2F-
human RKO cells NIPZWI1Rem:uaX\ldoF1cW:wIHHzd4F6 Mk[xRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCUS1:gZ4VtdHNuIFnDOVA:OiEQvF2= MonRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd|MEO0NlEoRjF5M{CzOFIyRC:jPh?=
human SW480 cells NVHwO2tNWHKxbHnm[ZJifGmxbjDhd5NigQ>? NGrrZllCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPXOFgxKGOnbHzzMEBKSzVyPUKuNkDPxE1? MoXhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd|MEO0NlEoRjF5M{CzOFIyRC:jPh?=
human SJSA1 cells NEfPe5VRem:uaX\ldoF1cW:wIHHzd4F6 MWTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOMU1GxJINmdGy|LDDJR|UxRTRwNUWg{txO M1fqTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF5M{CzOFIyLz5zN{OwN|QzOTxxYU6=
human HCT116 cells M4flZmN6fG:2b4jpZ:Kh[XO|YYm= M2m2dFUh\GG7cx?= Mn3QR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTGNVOTF4IHPlcIx{KGGodHXyJFUh\GG7czDifUBOXFNiYYPzZZnwxIxiSVO1NF0{NjJizszN NFfleIE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkOyOlE3QCd-MkKzNlYyPjh:L3G+
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ALL-PO NFiweVdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXfkTHQ{UW6qaXLpeIlwdiCxZjDoeY1idiCDTFytVG8h[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NEA:KDFwOUC4NVMh|ryPLh?= Mly2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMN|k{QTJ7Lze+V2FPT0WUPD;hQi=>
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MIA-PaCa-2 NYfyNJU3T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NVfKRnNnUW6qaXLpeIlwdiCxZjDoeY1idiCPSVGtVIFE[S1{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTBiPTC0PE45Ozh6IN88UU4> NFfSVmk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw{QTN7MkmvK|5USU6JRWK8M4E,
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Assay
Methods Test Index PMID
Western blot p-Cdk1 / Cdk1 / Cleaved PARP / Cleaved caspase-3 / p-p38 / Bad / Apaf1-1 / p-H2Ax / Bim / Bad 27385216
Immunofluorescence PARP1 / Plk1 28069876
Growth inhibition assay Cell viability 27385216

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)

激酶实验:[1]
  • CDK试验:

    CDK1 cyclin B1,CDK1 cyclin A,CDK2 cyclin E,和CDK4 cyclin D通过均相时间分辨荧光法在96孔格式中测量。实验缓冲液包含25 mM Hepes,6.25 mM MgCl2,0.003% Tween 20,0.3 mg/mL BSA,1.5 mM DTT,和如下含量的ATP: 162 μM (CDK1),90 mM (CDK2),或135 μM (CDK4)。CDK1和CDK2缓冲液包含10 mM MgCl2。测试化合物在20 μL实验缓冲液中稀释为它们终浓度的3倍,反应通过加入40 μL包含pRB底物(0.185μM)的试验缓冲液起始。板在37°C下连续搅拌培养30分钟,反应通过加入15 μL 含1.6μM 抗磷酸pRB抗体(Ser-780)的25 mM Hepes,24 mM EDTA,和0.2 mg/mL BSA终止。再振荡培育30分钟后,加入15μL 包含3nM Lance-Eu-W1024-labeledanti-rabbitIgG和60 nM Alophycocyanin共轭的抗-His-6 抗体的25 mM Hepes,以及0.5 mg/mL BSA,培育1小时。板在Victor-V多标阅读器上以340 nm激发波长和615 nm与665 nm发射波长读取数据。IC50值根据665 nm下的读数值进行计算,并归一化为615 nm下铕的读数值。Ki值根据公式Ki= IC50/(1 + S/Km )计算,其中S是试验中ATP浓度,Km是相对ATP的Michaelis-Menten常数。对激酶组的抑制活性通过IMAP测定技术确定。

细胞实验:[3]
  • Cell lines: MDA-MB-231 细胞系
  • Concentrations: 20 μM
  • Incubation Time: 72 h
  • Method: 对数生长期细胞(25,000)接种于96孔板,在37℃培养箱中与CO2一起培养,24小时后,给予不同浓度RO-3306以测定达到50%生长抑制(IC50)的药物浓度。MTT (20 μL,包含5mg/mL储备溶液的生理盐水)加入每孔中,细胞培养4小时。移除上清液,来自活细胞的甲瓒晶体溶解在200 μL无水DMSO中。吸光度使用550模式酶标仪在565 nm波长下检测。

溶解度(25°C)

体外

* 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 351.45
化学式

C18H13N3OS2

CAS号 872573-93-8
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

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操作手册

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