PD0166285

目录号：S8148 Purity: 99.59%

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

规格	价格	库存
10mM (1mL in DMSO)	1777.23	现货
5mg	1613.55	现货
25mg	5709.33	现货
100mg	12858.48	现货
1g	49058.75	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

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(PMID)
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。

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
激酶实验	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

参考文献
https://pubmed.ncbi.nlm.nih.gov/11719452/ https://pubmed.ncbi.nlm.nih.gov/17177986/ https://pubmed.ncbi.nlm.nih.gov/20832752/

参考文献

https://pubmed.ncbi.nlm.nih.gov/11719452/
https://pubmed.ncbi.nlm.nih.gov/17177986/
https://pubmed.ncbi.nlm.nih.gov/20832752/

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)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1年-80°C溶于溶剂
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1个月-20°C溶于溶剂

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 (195.14 mM)

Water : Insoluble

摩尔浓度计算器

体内溶解配方批次：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
均匀悬浊液	CMC-NA	≥5mg/ml	以 1 mL 工作液为例，取 5 mg该产品加到 1 ml CMC-NA 溶液中，混合均匀，即可得工作液浓度为 5 mg/ml的均匀悬浊液。
澄清溶液	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O 该配方已经过Selleck实验室实测。如果上述溶解方案不能满足您的需求，可联系Selleck销售提供定制化测试。	2.500mg/ml (4.88mM)	以 1 mL 工作液为例,取50μL50mg/ml的澄清DMSO储备液加到400μLPEG300中,混合均匀使其澄清;向上述体系中加入50μLTween80,混合均匀使其澄清;然后继续加入500μLddH2O定容至1mL。工作液请现配现用!
澄清溶液	5% DMSO 1 95% Corn oil 该配方已经过Selleck实验室实测。如果上述溶解方案不能满足您的需求，可联系Selleck销售提供定制化测试。	0.500mg/ml (0.98mM)	以1 mL工作液为例，取50μL 10mg/ml的澄清DMSO储备液加到950μL玉米油中，混合均匀。工作液请现配现用！

实验计算

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×

稀释计算器分子量计算器

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 μL 动物数量只

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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