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网站主页 化工产品目录 生物化工 生化试剂 激动剂抑制剂 6-(2,6-二氯苯基)-2-[[4-[2-(二乙基氨基)乙氧基]苯基]氨基]-8-甲基吡啶并[2,3-D]嘧啶-7(8H)-酮 化合物 PD0166285
  • 化合物 PD0166285|T6931|TargetMol

化合物 PD0166285|T6931|TargetMol

PD0166285
185039-89-8
￥496 1mg 起订
￥1190 5mg 起订
￥1930 10mg 起订
上海 更新日期：2024-09-29

TargetMol中国（陶术生物）

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联系人：邵小姐
手机：4008200310 拨打
邮箱：marketing@tsbiochem.com

产品详情:

中文名称：
化合物 PD0166285
英文名称：
PD0166285
CAS号：
185039-89-8
品牌：
TargetMol
产地：
美国
保存条件：
Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
纯度规格：
99.59%
产品类别：
抑制剂
货号：
T6931

Product Introduction

Bioactivity

名称PD0166285
描述PD0166285 is a potent Wee1 and Chk1 inhibitor with activity at nanomolar concentrations.PD0166285 is a novel G2 checkpoint abrogator.
细胞实验B16 cells (1 × 105 cells in 100 mm-dishes) are maintained in medium overnight. In addition, the cells are treated with (0, 0.5, 1.0, or 2.0 μM) PD0166285 (including DMSO vehicle) for indicated times. The cells are washed twice with phosphate-buffered saline (PBS). Next, the cells are trypsinized, so the cell numbers in each dish are determined by using a computed cell-counter (Sysmex CDA-500) according to manufacturer's recommendation. (Only for Reference)
激酶实验Wee1 Mass Screening: Wee1 mass screening is performed using Amersham's p34cdc2 kinase SPA kit with some modifications. Briefly, 45–60 nM full-length Wee1 kinase is incubated with 25 μM compounds, 20 μM ATP, and 122–441 nM Cdc2/cyclin B in a final volume of 50 μl of enzyme dilution buffer [50 mM Tris (pH 8.0), 10 mM NaCl, 10 mM MgCl2, 1 mM DTT, and 0.1 mM Na3VO4]. After 30 min incubation at 30°C, 30 μl of [33P]ATP containing kinase buffer [67 mM Tris (pH 8.0), 40 mM NaCl, 13 mM MgCl2, 1 mM DTT, and 0.13 mM Na3VO4] containing 1 μM biotinylated peptide, and 0.25 μCi of [γ-33P]ATP is added to the reaction and incubated for another 30 min at 30°C. The reaction is stopped by adding 200 μl of stop buffer [50 μM ATP, 5 mM EDTA, 0.1% Triton X-100, and 1.25 mg/ml SPA beads in PBS]. After centrifugation at 2400 rpm for 15 min, the plate is counted with Wallac's Microbeta counter.
动物实验E98 tumor fragments (8 mm3) were grafted subcutaneously in the flank of Balb/C nude mice (n = 10). For the experiments with the orthotopic tumors, U251 mg and E98 cells were transduced to express Fluc and mCherry, to generate U251-FM and E98-FM cells. One million cells were injected intracranially. Starting at 12 days after tumor inoculation, mice received the WEE1 inhibitor PD0166285 via intraperitoneal injections (500 μl of a 20 μM solution diluted in NaCl) or vehicle for 5 consecutive days. On days 10–15, mice were irradiated with a single dose of irradiation.
体外活性PD0166285通过纳摩尔浓度抑制Wee1活性，使G2/M检查点失效，诱导提前细胞分裂。在细胞水平上，0.5 μM PD0166285显著抑制七种测试癌细胞系中的辐射诱导的Cdc2在Tyr-15和Thr-14的磷酸化。PD0166285通过废除G2检查点来杀死癌细胞。PD0166285不抑制Cdc2/cyclin B，而是以更高浓度（3433 nM）抑制Chk1激酶。用抑制剂治疗细胞与微管稳定和cyclin D转录减少有关。因此，PD0166285可能是一种有潜力的抗癌疗法[1][2]。
体内活性PD0166285在0.5 μM浓度下，能够抑制所有测试细胞系中的Cdc2Y15/T14磷酸化，这一效果与细胞的p53状态无关[1]。此外，通过药理学上靶向WEE1的PD0166285能够增强U251-FM GBM肿瘤对体内IR的敏感性[3]。
存储条件Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度Ethanol : 93 mg/mL (181.5 mM)
DMSO : 93 mg/mL (181.5 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)
关键字PD 166285 | Wee1 | Inhibitor | inhibit | PD0166285 | Apoptosis | PD166285 | PD-0166285 | PD 0166285
相关产品L-Glutamic acid | Metronidazole | 5-Fluorouracil | Dextran sulfate sodium salt (MW 4500-5500) | Stavudine | Tributyrin | Myricetin | Sorafenib | L-Ascorbic acid | Acetylcysteine | Salicylic acid | Sodium 4-phenylbutyrate
相关库抑制剂库 | 经典已知活性库 | 抗癌化合物库 | 已知活性化合物库 | 细胞周期化合物库 | 激酶抑制剂库 | 细胞凋亡化合物库 | 抗衰老化合物库 | NO PAINS 化合物库 | 表型筛选靶点鉴定库
PD-166285|TargetMol

公司简介

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。 凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

成立日期 (12年)
注册资本 566.265100万人民币
员工人数 100-500人
年营业额 ￥ 1亿以上
经营模式 贸易,工厂,试剂,定制,服务
主营行业 天然产物,生化试剂,分子生物学,分子砌块,生物技术服务

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