PD0166285
PD0166285 是一种有效的 Wee1 和 Chk1 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
CAS: 185039-89-8
产品质控
PD0166285相关产品
| 相关产品 | Adavosertib (MK-1775) | 点击展开 |
|---|---|---|
| 相关化合物库 | 激酶抑制剂库 PI3K/Akt 抑制剂库 MAPK抑制剂库 DNA损伤/ DNA修复化合物库 细胞周期化合物库 | 点击展开 |
相关信号通路图
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 Wee1 和 Chk1 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。 | ||||||
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| 靶点 |
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| 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。 |
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| 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 |
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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) | |||
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体外溶解度 |
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 (195.14 mM) Water : Insoluble |
摩尔浓度计算器 |
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体内溶解度 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
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
只
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，注：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：取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：取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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