化合物 AZD7762|T6093|TargetMol

AZD-7762
860352-01-8

￥273 1mg 起订

￥385 2mg 起订

￥592 5mg 起订

上海更新日期：2024-12-12

TargetMol中国（陶术生物）

VIP3年

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 AZD7762

英文名称：: AZD-7762

CAS号：: 860352-01-8

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：: 99.19%

产品类别：: 抑制剂

货号：: T6093

Product Introduction

Bioactivity

名称	AZD-7762
描述	AZD-7762, an effective and specific inhibitor of Chk1（IC50=5 nM）, is equally potent against Chk2 and less potent against CAM, Yes, Fyn, Lyn, Hck and Lck.
细胞实验	For the checkpoint abrogation assay, HT29 cells are treated for 2 hours with camptothecin (topoisomerase I inhibitor; 0.07 μg/mL) to induce the G2 checkpoint. Cells are then treated for 20 hours with a 12-point titration of AZD7762 (12.5 μM to 6 nM) plus nocodazole. Cells are fixed with 3.7% formaldehyde for 1 hour, permeabilized with PBS containing 0.05% Triton X, and incubated with anti-phH3 antibody for 1 hour followed by Alexa Fluor 488 anti-rabbit and Hoechst stain for 1 hour. Mitotic index is determined on the ArrayScan and expressed as the percentage of cells undergoing mitosis. For the potentiation assays, SW620 or MDA-MB-231 cells are dosed for 24 hours with a 9-point titration of gemcitabine ranging from 0.01 to 100 nM with a constant dose of AZD7762 (300 nM). After 24 hours, medium is removed and AZD7762 alone is added back to the wells for an additional 24 hours. Cells are then incubated in AZD7762-free medium for an additional 72 hours. The effect on cell proliferation is determined by MTT.(Only for Reference)
激酶实验	Chk1 Kinase Assay: Recombinant human Chk1 is expressed as a glutathione S-transferase fusion in insect cells using a baculovirus vector and purified by glutathione affinity chromatography. A synthetic peptide substrate (N-biotinylaminohexanoyl-KKVSRSGLYRSPMPENLNRPR) for Chk1 is synthesized. Final assay concentrations of peptide and ATP (cold + 40 nCi [33P]ATP) are 0.8 and 1 μM, respectively. Different concentrations of AZD7762, buffer containing peptide and chk1 kinase and ATP, are added sequentially to a 384-well assay plate. The plate is incubated for 2 hours, reaction is stopped by the addition of buffer containing EDTA and scintillation proximity assay beads, and plates are read using a TopCount reader. Data analysis is carried out to determinate a dose response (IC50).
体外活性	AZD7762，作为一种选择性更强的Chk1抑制剂，通过可逆地结合到Chk1的ATP结合位点，抑制cdc25C肽的Chk1磷酸化作用，其IC50为5 nM，Ki为3.6 nM。AZD7762以EC50为0.620 μM的浓度引起细胞阻滞，并且通过阻断chk1依赖的Cdc25A降解和Cyclin A激活，显著消除了以EC50为10 nM的浓度的喜树碱诱导的G2阶段阻滞。在300 nM浓度下，AZD7762增强了对SW620细胞的吉西他滨和对MDA-MB-231细胞的拓扑替康的抗肿瘤效果，将GI50值分别从24.1 nM和2.25 μM减少到1.08 nM和0.15 μM。[1] AZD7762还对携带p53野生型、p53突变、Mdm2扩增或p14缺失的多种神经母细胞瘤细胞系显示出IC50值在82.6-505.9 nM范围内的细胞毒性。[2]
体内活性	AZD7762以25 mg/kg的剂量，在H460-DNp53移植小鼠和SW620移植小鼠中几乎不显示出抗肿瘤活性；但与吉西他滨（60 mg/kg）联合应用时，在两种移植小鼠中表现出显著的抗肿瘤效果，低剂量（12.5 mg）下的细胞杀伤量为0.9或治疗对照组百分比（%T/C）为26。在H460-DNp53移植大鼠中，AZD7762与吉西他滨（10 mg/kg）联合给药能够以剂量依赖性方式抑制肿瘤体积，10和20 mg/kg AZD7762的%T/C值分别为48和32。在与伊立替康（25或50 mg/kg）联合应用时，AZD7762（25 mg/kg）能够使SW620移植小鼠中的肿瘤完全消退，%T/C值显著增加至-66%和-67%。[1]
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 : < 1 mg/mL (insoluble or slightly soluble) DMSO : 47 mg/mL (129.7 mM) H2O : < 1 mg/mL (insoluble or slightly soluble)
关键字	Checkpoint Kinase (Chk) \| AZD-7762 \| inhibit \| Inhibitor \| AZD 7762
相关产品	BX795 \| ANI-7 \| Prexasertib dihydrochloride \| CCT241533 hydrochloride \| Prexasertib \| Rabusertib \| CHK1-IN-4 hydrochloride \| CCT245737 \| Baricitinib \| CHK1-IN-3 \| PD0166285 \| A-443654
相关库	抑制剂库 \| 抗癌活性化合物库 \| 经典已知活性库 \| 已知活性化合物库 \| ReFRAME 相关化合物库 \| 激酶抑制剂库 \| 临床期小分子药物库 \| 药物功能重定位化合物库 \| 抗癌临床化合物库 \| 抗癌药物库

AZD7762|TargetMol

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