PD0166285

PD0166285 是一种有效的 Wee1Chk1 抑制剂,对Wee1和Myt1的IC50值分别为24 nM和72 nM。PD0166285 也是一种新型的G2检查点的抑制剂。PD0166285 可诱导凋亡。

PD0166285 Chemical Structure

PD0166285 Chemical Structure

CAS: 185039-89-8

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 1777.23 现货
5mg RMB 1613.55 现货
25mg RMB 5709.33 现货
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产品质控

批次: S814801 DMSO] 100 mg/mL] false] Ethanol] 100 mg/mL] false] Water] Insoluble] false 纯度: 99.59%
99.59

PD0166285相关产品

相关信号通路图

Wee1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
MCF-7 Function assay 12 mg/kg Weight change of MCF-7 tumor cells in mice at 12 mg/kg peroral dose, days 1-15 administration 9703473
RAVSMCs Function assay 2 hr Inhibition of PDGF-stimulated Platelet-derived growth factor receptor autophosphorylation in rat aortic vascular smooth muscle cells (RAVSMCs) after 2 hr, IC50=0.0065μM 9784112
C6 Function assay 2 hr Inhibition of PDGF-stimulated Platelet-derived growth factor receptor autophosphorylation in C6 rat glioma cells after 2 hr, IC50=0.005μM 9784112
MDA-MB-231 Antiproliferative assay 72 hrs Antiproliferative activity against human MDA-MB-231 cells measured after 72 hrs by CellTiter-Blue assay, IC50=0.16μM 28792760
HEK293T Antiproliferative assay 72 hrs Antiproliferative activity against HEK293T cells measured after 72 hrs by CellTiter-Blue assay, IC50=0.29μM 28792760
MM1S Antiproliferative assay 72 hrs Antiproliferative activity against human MM1S cells measured after 72 hrs by CellTiter-Blue assay, IC50=0.52μM 28792760
C6 Function assay Inhibition of PDGF-induced autophosphorylation of PDGF-R in C6 cells, IC50=0.005μM 9703473
NIH3T3 Function assay Inhibition of PDGF-induced autophosphorylation of PDGF-R in NIH3T3 cells, IC50=0.0018μM 9703473
SW-620 Function assay Inhibitory activity against SW-620 human colon adenocarcinoma cells was determined, IC50=0.27μM 10956222
HT-29 Function assay Inhibitory activity against HT-29 human colon adenocarcinoma cells was determined, IC50=0.28μM 10956222
HCT-8 Function assay Inhibitory activity against HCT-8 human colon adenocarcinoma cells was determined, IC50=0.42μM 10956222
HEK293 Function assay Binding affinity to human full-length His-tagged Myt1 kinase expressed in HEK293 cells by TR-FRET based binding assay, IC50=0.0072μM 22770610
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
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 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
U-2 OS qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 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
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 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
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 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
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells 29435139
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells 29435139
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) 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
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells 29435139
Rh30 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells 29435139
HEK293 qHTS assay Inhibition of human full length PKMYT1 expressed in HEK293 cells using EFS (247 to 259 residues) as substrate after 1 hr by fluorescence polarization immunoasay, Ki=0.0008μM 29941193
HEK293 qHTS assay Inhibition of human full length PKMYT1 expressed in HEK293 cells using EFS (247 to 259 residues) as substrate after 1 hr by fluorescence polarization immunoasay, IC50=0.008μM 29941193
点击查看更多细胞系数据

生物活性

产品描述 PD0166285 是一种有效的 Wee1Chk1 抑制剂,对Wee1和Myt1的IC50值分别为24 nM和72 nM。PD0166285 也是一种新型的G2检查点的抑制剂。PD0166285 可诱导凋亡。
靶点
Wee1 [1]
(Cell-free assay)
Myt1 [1]
(Cell-free assay)
Chk1 [1]
(Cell-free assay)
24 nM 72 nM 3.4 μM
体外研究(In Vitro)
体外研究活性 PD0166285在微摩尔浓度下便可抑制Wee1的活性,它取消了G2/M期DNA损伤检验点、致使细胞进入早期细胞分裂(尚未进行DNA损伤修复)。在七种检测到的癌细胞株上,0.5 μM的PD0166285显著抑制放射诱导的Cdc2磷酸化(pTyr-15和pThr-14)。PD0166285能使细胞跳过G2/M期DNA损伤检验点从而诱使细胞进入早期分裂、凋亡可用来杀死癌细胞。PD0166285对Cdc2/cyclin B没有抑制作用,但在较高浓度下(3433 nM)可抑制Chk1。对细胞以PD0166285处理可抑制cyclin D转录并与微管稳定性相关[1][2]
激酶实验 Wee1 Mass Screening
45–60 nM 全长Wee1激酶用含25 μM化合物, 20 μM ATP以及122-441 nM Cdc2/cyclin B的50 μl enzyme dilution buffer进行孵育. 在30°C孵育30分钟后, 将包含1μM biotinylated peptide, 0.25 μCi of [γ-33P]ATP的30 μl kinase buffer(67 mM Tris (pH 8.0), 40 mM NaCl, 13 mM MgCl2, 1 mM DTT, and 0.13 mM Na3VO4)和1μM biotinylated peptide, 0.25 μCi of [γ-33P]加入反应体系,在30°C再孵育30分钟。通过在反应体系中加入200 μl的stop buffer以终止反应。2400 rpm离心15分钟, 在Wallac’s Microbeta counter对平板进行计数。
细胞实验 细胞系 B16小鼠黑色素瘤细胞
浓度 0.5, 1, 2 μM
孵育时间 4小时,24小时
方法

B16细胞在培养基中培养过夜。予以这些细胞(0, 0.5, 1.0, or 2.0 μM)PD0166285进行不同时间的处理,处理完后,用PBS洗涤两次。胰蛋白酶化这些细胞并进行细胞计数。

实验图片 检测方法 检测指标 实验图片 PMID
Western blot p-Cdc2 / Cdc2 / Wee1 / Cyclin B 17177986
Immunofluorescence Wee1 / α-tubulin 17177986
体内研究(In Vivo)
体内研究活性 PD0166285抑制Wee1在体内可使U251-FM恶性胶质瘤对辐射敏感[3]
动物实验 Animal Models 携带移植的恶性胶质瘤细胞的裸鼠
Dosages 0, 20, 100, 200, or 400 µM in 100 µl
Administration 皮下注射

化学信息&溶解度

分子量 512.43 分子式

C26H27Cl2N5O2

CAS号 185039-89-8 SDF Download PD0166285 SDF
Smiles CCN(CC)CCOC1=CC=C(C=C1)NC2=NC=C3C=C(C(=O)N(C3=N2)C)C4=C(C=CC=C4Cl)Cl
储存条件(自收到货起)

体外溶解度
批次:

DMSO : 100 mg/mL ( (195.14 mM); DMSO吸湿会降低化合物溶解度,请使用新开封DMSO)

Ethanol : 100 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。

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