Monastrol

别名: (±)-Monastrol

此产品请避光密封保存。

Monastrol ((±)-Monastrol)是一种具有细胞透性的kinesin-5(KIF11)小分子抑制剂,IC50为14μM,kinesin-5(KIF11)可保持半纺锤体的分离状态。

Monastrol Chemical Structure

Monastrol Chemical Structure

CAS: 329689-23-8

规格 价格 库存 购买数量
10mg RMB 1204.01 现货
50mg RMB 4070.85 现货
更大包装 有超大折扣

400-668-6834

info@selleck.cn

免费分装
免费预溶

客户使用Selleck的发表文献11

产品质控

批次: 纯度: 99.86%
99.35

Monastrol相关产品

相关信号通路图

Kinesin抑制剂选择性比较

细胞实验数据示例

细胞系 实验类型 给药浓度 孵育时间 活性描述 文献信息
C6 Antiproliferative assay 100 uM 24 hrs Antiproliferative activity against rat C6 cells assessed as reduction in cell viability at 100 uM after 24 hrs by MTS assay relative to control ChEMBL
C6 Cell cycle assay 100 uM 24 hrs Cell cycle arrest in rat C6 cells assessed as accumulation at G2/M phase at 100 uM after 24 hrs by propidium iodide staining based flow cytometry ChEMBL
U138MG Apoptosis assay 200 uM 48 hrs Induction of apoptosis in human U138MG cells at 200 uM after 48 hrs by Annexin V/propidium iodide staining based flow cytometry ChEMBL
U138MG Necrosis assay 200 uM 48 hrs Induction of necrosis in human U138MG cells at 200 uM after 48 hrs by Annexin V/propidium iodide staining based flow cytometry ChEMBL
C6 Apoptosis assay 100 uM 48 hrs Induction of apoptosis in rat C6 cells at 100 uM after 48 hrs by Annexin V/propidium iodide staining based flow cytometry ChEMBL
U138MG Function assay 200 uM 24 hrs Inhibition of EG5 in human U138MG cells assessed as monopolar spindle formation at 200 uM after 24 hrs by Hoechst staining based immunofluorescence microscopic method ChEMBL
C6 Function assay 100 uM 24 hrs Inhibition of EG5 in rat C6 cells assessed as monopolar spindle formation at 100 uM after 24 hrs by Hoechst staining based immunofluorescence microscopic method ChEMBL
C6 Antiproliferative assay 5 to 50 uM 48 hrs Antiproliferative activity against rat C6 cells at 5 to 50 uM after 48 hrs by Neubauer chamber method ChEMBL
MCF7 Antiproliferative assay 25 uM 48 hrs Antiproliferative activity against human MCF7 cells at 25 uM after 48 hrs by sulforhodamine B assay ChEMBL
NCI/ADR-RES Antiproliferative assay 25 uM 48 hrs Antiproliferative activity against human NCI/ADR-RES cells at 25 uM after 48 hrs by sulforhodamine B assay ChEMBL
786-0 Antiproliferative assay 25 uM 48 hrs Antiproliferative activity against human 786-0 cells at 25 uM after 48 hrs by sulforhodamine B assay ChEMBL
HT-29 Antiproliferative assay 25 uM 48 hrs Antiproliferative activity against human HT-29 cells at 25 uM after 48 hrs by sulforhodamine B assay ChEMBL
UACC62 Antiproliferative assay 25 uM 48 hrs Antiproliferative activity against human UACC62 cells at 25 uM after 48 hrs by sulforhodamine B assay ChEMBL
PC3 Antiproliferative assay 25 uM 48 hrs Antiproliferative activity against human PC3 cells at 25 uM after 48 hrs by sulforhodamine B assay ChEMBL
OVCAR3 Antiproliferative assay 25 uM 48 hrs Antiproliferative activity against human OVCAR3 cells at 25 uM after 48 hrs by sulforhodamine B assay ChEMBL
KBV1 Antiproliferative assay 72 hrs Antiproliferative activity against human KBV1 cells overexpressing MDR1 after 72 hrs by Alamar blue assay in presence of zosuquidar, EC50=45.394μM 20597485
hTERT-HME1 Antiproliferative assay 72 hrs Antiproliferative activity against human hTERT-HME1 cells after 72 hrs by Alamar blue assay, EC50=45.082μM 20597485
HCT116 Antiproliferative assay 72 hrs Antiproliferative activity against human HCT116 cells after 72 hrs by Alamar blue assay, EC50=24.155μM 20597485
HeLa Function assay 12 hrs Inhibition of Eg5 ATPase activity expressed in HeLa cells after 12 hrs, IC50=6.1μM 17587586
HL-60(TB) Growth inhibition assay 24 hrs Growth inhibition of human HL-60(TB) cells incubated for 24 hrs by MTT assay, IC50=0.147μM 28667871
MOLT4 Growth inhibition assay 24 hrs Growth inhibition of human MOLT4 cells incubated for 24 hrs by MTT assay, IC50=0.215μM 28667871
McCoy Cytotoxicity assay 72 hrs Cytotoxicity against mouse McCoy cells assessed as decrease in cell viability after 72 hrs by MTT assay, IC50=26.8μM 29908443
MM1S Antiproliferative assay 72 hrs Antiproliferative activity against human MM1S cells incubated for 72 hrs by MTT assay, IC50=8.7μM ChEMBL
HCT116 Antiproliferative assay 72 hrs Antiproliferative activity against human HCT116 cells incubated for 72 hrs by MTT assay, IC50=9μM ChEMBL
CCRF-CEM Growth inhibition assay Growth inhibition of human CCRF-CEM cells, GI50=31.6μM 21855351
M14 Growth inhibition assay Growth inhibition of human M14 cells, GI50=25.1μM 21855351
HL-60(TB) Growth inhibition assay Growth inhibition of human HL-60(TB) cells, GI50=25.1μM 21855351
KBV1/KB3-1 Function assay Drug resistant ratio of EC50 for human KBV1 cells overexpressing MDR1 to EC50 for KB3-1 cells, EC50=0.0012μM 20597485
HCT116 Cell cycle assay Effect on cell cycle progression in human HCT116 cells assessed as increase in phospho-histone H3 by fluorescence microscopy, EC50=1.5μM 18793847
HCT116 Cell cycle assay Effect on cell cycle progression in human HCT116 cells assessed as mitotic arrest measured by doubling DNA content by fluorescence microscopy, EC50=1.2μM 18793847
K562 Growth inhibition assay Growth inhibition of human K562 cells, GI50=31.6μM 21855351
MOLT4 Growth inhibition assay Growth inhibition of human MOLT4 cells, GI50=31.6μM 21855351
SR Growth inhibition assay Growth inhibition of human SR cells, GI50=31.6μM 21855351
NCI-H522 Growth inhibition assay Growth inhibition of human NCI-H522 cells, GI50=31.6μM 21855351
COLO205 Growth inhibition assay Growth inhibition of human COLO205 cells, GI50=31.6μM 21855351
HCT116 Growth inhibition assay Growth inhibition of human HCT116 cells, GI50=31.6μM 21855351
KM12 Growth inhibition assay Growth inhibition of human KM12 cells, GI50=31.6μM 21855351
SF295 Growth inhibition assay Growth inhibition of human SF295 cells, GI50=31.6μM 21855351
U251 Growth inhibition assay Growth inhibition of human U251 cells, GI50=31.6μM 21855351
SK-MEL-2 Growth inhibition assay Growth inhibition of human SK-MEL-2 cells, GI50=31.6μM 21855351
RPMI8266 Growth inhibition assay Growth inhibition of human RPMI8266 cells, GI50=31.6μM 21855351
NCI-H322M Growth inhibition assay Growth inhibition of human NCI-H322M cells, GI50=39.8μM 21855351
HCC2998 Growth inhibition assay Growth inhibition of human HCC2998 cells, GI50=39.8μM 21855351
HCT15 Growth inhibition assay Growth inhibition of human HCT15 cells, GI50=39.8μM 21855351
SW620 Growth inhibition assay Growth inhibition of human SW620 cells, GI50=39.8μM 21855351
SNB75 Growth inhibition assay Growth inhibition of human SNB75 cells, GI50=39.8μM 21855351
SK-MEL-5 Growth inhibition assay Growth inhibition of human SK-MEL-5 cells, GI50=39.8μM 21855351
UACC62 Growth inhibition assay Growth inhibition of human UACC62 cells, GI50=39.8μM 21855351
SN12C Growth inhibition assay Growth inhibition of human SN12C cells, GI50=39.8μM 21855351
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells 29435139
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells 29435139
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells 29435139
U-2 OS qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells 29435139
点击查看更多细胞系数据

生物活性

产品描述 Monastrol ((±)-Monastrol)是一种具有细胞透性的kinesin-5(KIF11)小分子抑制剂,IC50为14μM,kinesin-5(KIF11)可保持半纺锤体的分离状态。
靶点
KIF11(Eg5) [4]
(Cell-based assay)
14 μM
体外研究(In Vitro)
体外研究活性

Monastrol并不是通过细胞周期的S期和G2期或中心体复制抑制细胞周期进程。monastrol的有丝分裂阻滞作用快速可逆。它还能在爪蟾卵提取物中抑制双极纺锤体的形成。Monastrol将细胞阻滞在有丝分裂期,但在体外不影响处于有丝分裂间期细胞的微管或是微管聚合[1]。将交感神经元细胞暴露于monastrol几小时,将会增加轴突数量及生长速率。但时间延长,轴突的总体长度则与对照组无异。感觉神经元同样也有这种轴突生长速率短期升高的效果,然而,进一步延长暴露时间将导致轴突变短,说明感觉神经元细胞对药物的毒性作用更为敏感。但是,细胞整体培养状况比taxol处理组要更为强健,taxol是一种常用于治疗癌症的药物[2]。在HeLa细胞中,monastrol激活纺锤体检验点,导致有丝分裂受到阻滞,引起凋亡[3]

细胞实验 细胞系 BS-C-1 (猴肾脏上皮)细胞
浓度 100 μM
孵育时间 4 h
方法

在胸腺嘧啶脱氧核苷双重阻滞实验中,处于生长对数期的BS-C-1细胞在含2 mM胸苷的正常培养基中培养。然后将细胞置于含24 μM deoxycytidine的培养基中培养9小时。第二次阻滞时,将细胞至于要含2 mM 胸苷的无血清培养基中16小时。最后,将细胞重新置于含24 μM deoxycytidine的培养基中,加入100 μM monastrol或0.1% DMSO。为了检测monastrol和nocodazole的作用是否具有可逆性。将BS-C-1铺于盖玻片上,用含2 μM nocodazole或是100 μM monastrol的正常生长培养基处理4小时,然后将细胞置于正常培养基。在不同的时间节点,将盖玻片进行免疫荧光染色,对处于有丝分裂间期或有丝分裂期的细胞进行计数。

实验图片 检测方法 检测指标 实验图片 PMID
Growth inhibition assay Cell viability 26035434
Western blot Cyclin B / Survivin 26035434

化学信息&溶解度

分子量 292.35 分子式

C14H16N2O3S

CAS号 329689-23-8 SDF Download Monastrol SDF
Smiles CCOC(=O)C1=C(NC(=S)NC1C2=CC(=CC=C2)O)C
储存条件(自收到货起) 3年 -20°C(避光) 粉状

体外溶解度
批次:

DMSO : 58 mg/mL ( 198.39 mM; DMSO吸湿会降低化合物溶解度,请使用新开封DMSO)

Ethanol : 58 mg/mL

Water : Insoluble

摩尔浓度计算器

体内溶解度
批次:

现配现用,请按从左到右的顺序依次添加,澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量 浓度 体积 分子量

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。

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

请输入您的姓名
请输入您的邮箱地址 请输入一个有效的邮箱地址
请写点东西给我们
Tags: buy Monastrol | Monastrol supplier | purchase Monastrol | Monastrol cost | Monastrol manufacturer | order Monastrol | Monastrol distributor
在线咨询
联系我们