Ro-3306

For research use only. Not for use in humans.

目录号:S7747

Ro-3306 Chemical Structure

CAS No. 872573-93-8

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。

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
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客户使用Selleck生产的Ro-3306发表文献80篇:

产品安全说明书

CDK抑制剂选择性比较

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 NX3idpdkeUiWUzDhd5NigQ>? NHHrSFlRNWeueXPvdJJwfGWrbjDzeYJ{fHKjdHXzJIll\W62aX\p[YQhcW5iS1KtN{0yKGGmZX7vZ4Fz[2mwb33hJINmdGxibHnu[UwheUiWUzD0bIVz[XCndYTpZ{BtcWK{YYL5JJNkemWnbh?= M1fhbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNzNUG1Nlg1Lz5|MUWxOVI5PDxxYU6=
human H460a cells MUXQdo9tcW[ncnH0bY9vKGG|c3H5 M1WyWGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSES2NIEh[2WubIOsJGlEPTB;MT6wOEDPxE1? NHjQfHY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{OwN|QzOSd-MUezNFM1OjF:L3G+
human MDA435 cells Mn7LVJJwdGmoZYLheIlwdiCjc4PhfS=> MkTJRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPRFG0N|Uh[2WubIOsJGlEPTB;MT6xOEDPxE1? NFTFRVM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{OwN|QzOSd-MUezNFM1OjF:L3G+
human HCT116 cells NI\NWlVRem:uaX\ldoF1cW:wIHHzd4F6 MYDBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiFVEGxOkBk\WyuczygTWM2OD1zLkG0JO69VQ>? Mmn4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd|MEO0NlEoRjF5M{CzOFIyRC:jPh?=
human RKO cells NXjkNWRSWHKxbHnm[ZJifGmxbjDhd5NigQ>? M{W5W2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iUlvPJINmdGy|LDDJR|UxRTJizszN MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzNyM{SyNUc,OTd|MEO0NlE9N2F-
human SW480 cells NHHhZWRRem:uaX\ldoF1cW:wIHHzd4F6 NF;IVXJCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPXOFgxKGOnbHzzMEBKSzVyPUKuNkDPxE1? MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPzNyM{SyNUc,OTd|MEO0NlE9N2F-
human SJSA1 cells NXzrSJRsWHKxbHnm[ZJifGmxbjDhd5NigQ>? NWXoO2dpSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTTnNCOSClZXzsd{whUUN3ME20MlU2KM7:TR?= MkXyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTd|MEO0NlEoRjF5M{CzOFIyRC:jPh?=
human HCT116 cells NV7WeoN6S3m2b4TvfIlkyqCjc4PhfS=> M2HlTlUh\GG7cx?= MW\DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh[W[2ZYKgOUBl[Xm|IHL5JG1VWyCjc4Phfg+9lCCLQ{WwQVMvOiEQvF2= MoLOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ|Mk[xOlgoRjJ{M{K2NVY5RC:jPh?=
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C-33-A NXPvcXhJT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mlr3TY5pcWKrdHnvckBw\iCqdX3hckBENTN|LVGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3MDC9JFQ5Njd3NUSg{txONg>? MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyzPVM6OjlxJ{7TRW5ITVJ:L3G+
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HCC1954 M3e2TWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M2LjbmlvcGmkaYTpc44hd2ZiaIXtZY4hUEOFMUm1OEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwJF0hPDlwMEi3NUDPxE1w NXi2RVA5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOzl|OUK5M{c,W0GQR1XSQE9iRg>?
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RKO NYPke4psT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NFriUGdKdmirYnn0bY9vKG:oIHj1cYFvKFKNTzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyIE2gOFkvQDN3NjFOwG0v MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyzPVM6OjlxJ{7TRW5ITVJ:L3G+

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-Cdk1 / Cdk1 / Cleaved PARP / Cleaved caspase-3 / p-p38 / Bad / Apaf1-1 / p-H2Ax / Bim / Bad; 

PubMed: 27385216     


OVCA-429 and OVCAR-3 were exposed to RO-3306 for 24 h in indicated dose dependent manner, (F) 10 uM RO-3306 for 12 h up to 48 h. The expression level of the indicated protein and the phosphorylated form of H2A.x and p38 were examined via Western blot analyses.

27385216
Immunofluorescence
PARP1 / Plk1 ; 

PubMed: 28069876     


Representative images of IF staining for PARP1 and Plk1 in 22RV1 cells treated with 0.3 mM mimosine for 20 h, 4 mM hydroxyurea for 24 h, 10 µM RO-3306 for 7 h or 200 ng/ml nocodazole (Noc) for 12 h.

28069876
Growth inhibition assay
Cell viability; 

PubMed: 27385216     


OVCA-429 and OVCAR-3 were exposed to RO-3306 in indicated time- and dose-dependent manner. Cell viability were measured via crystal violet assay. Results are the means ± S.E. n = 3. 

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]
- 合并

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]
- 合并
  • 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。
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 13 mg/mL warmed (36.98 mM)
Water Insoluble
Ethanol Insoluble

* 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 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

CDK Signaling Pathway Map

相关CDK产品

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID