阿贝司他|T0431|TargetMol

Abexinostat
783355-60-2

￥276 1mg 起订

￥389 2mg 起订

￥663 5mg 起订

上海更新日期：2024-12-12

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：: 阿贝司他

英文名称：: Abexinostat

CAS号：: 783355-60-2

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：: 98.43%

产品类别：: 抑制剂

货号：: T0431

Product Introduction

Bioactivity

名称	Abexinostat
描述	PCI-24781 (Abexinostat (PCI24781)) is a new pan-HDAC inhibitor mainly targeting HDAC1 (Ki: 7 nM), also have moderate inhibitory for HDACs 2, 3, 6, and 10 and greater than 40-fold selectivity against HDAC8. Phase 1/2.
细胞实验	Cells are cultured for at least two doubling times, and growth is monitored at the end of PCI-24781 exposure using an Alamar blue fluorometric cell proliferation assay. PCI-24781 is assayed in triplicate wells in 96-well plates at nine concentrations using half-log intervals ranging from 0.0015 μM to 10 μM. The final DMSO concentration in each well is 0.15%. The concentration required to inhibit cell growth by 50% (GI50) and 95% confidence intervals are estimated from nonlinear regression using a four-parameter logistic equation.(Only for Reference)
激酶实验	HDAC Activity: HDAC activity is measured using a continuous trypsin-coupled assay. For inhibitor characterization, measurements are done in a reaction volume of 100 μL using 96-well assay plates. For each isozyme, the HDAC protein in reaction buffer [50 mM HEPES, 100 mM KCl, 0.001% Tween 20, 5% DMSO (pH 7.4), supplemented with bovine serum albumin at concentrations of 0% (HDAC1), 0.01% (HDAC2, 3, 8, and 10), or 0.05% (HDAC6)] is mixed with PCI-24781 at various concentrations and allowed to incubate for 15 minutes. Trypsin is added to a final concentration of 50 nM, and acetyl-Gly-Ala-(N-acetyl-Lys)-AMC is added to a final concentration of 25 μM (HDAC1, 3, and 6), 50 μM (HDAC2 and 10), or 100 μM (HDAC8) to initiate the reaction. Negative control reactions are done in the absence of PCI-24781 in replicates of eight. Reactions are monitored in a fluorescence plate reader. After a 30-minute lag time, the fluorescence is measured over a 30-minute time frame using an excitation wavelength of 355 nm and a detection wavelength of 460 nm. The increase in fluorescence with time is used as the measure of the reaction rate. Inhibition constants Ki(app) are obtained using the program BatchKi.
体外活性	每星期连续四天给药三天不给药处理HCT116移植小鼠模型,给药浓度分别为20 mg/kg, 40 mg/kg, 80 mg/kg和160 mg/kg PCI-24781,抑制效果分别是48%, 57%, 82.2%,和80.0%.隔一天一次200 mg/kg PCI-24781作用于移植小鼠,HCT116 和 DLD-1肿瘤细胞生长受到明显抑制,抑制效果分别是69%和59%.
体内活性	在CHO细胞中,PCI-24781与抑制HR效果一致,导致同源定向修复（I-SceI诱导染色质断裂引起）能力下降。PCI-24781对多种肿瘤细胞系均有明显的抗肿瘤活性,GI50范围为0.15 μM~3.09 μM。PCI-24781处理使HCT116和DLD-1细胞系中组蛋白/微管蛋白乙酰化呈剂量依赖性积累,同时诱导PARP的剪切,p21表达和γH2AX累积。PCI-24781诱导软组织细胞的凋亡,引起S期缺失和G2期细胞周期停滞。在STS细胞中,PCI-24781极可能通过增强E2F1在Rad51近端启动子区域的结合诱导Rad51 转录抑制。PCI-24781还诱导非霍奇金淋巴瘤和Hodgkin淋巴瘤中蛋白酶和活性氧依赖的NF-κB信号通路介导的细胞凋亡过程。PCI-24781也抑制人脐静脉内皮细胞内皮细胞的增值,GI50为0.43 μM。PCI-24781抑制HDACs酶活导致HR 相关基因的转录水平出现明显下降,其中包括RAD51。
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	DMSO : 74 mg/mL (186.2 mM) Ethanol : < 1 mg/mL (insoluble or slightly soluble)
关键字	CRA-24781 \| CRA-024781 \| CRA24781 \| antitumor activity \| Inhibitor \| HDAC \| Abexinostat \| MBLAC2 \| inhibit \| CRA024781 \| Histone deacetylases
相关产品	Valproic acid sodium salt \| 4-Phenylbutyric acid \| Valproic Acid \| Panobinostat \| Methyl L-histidinate dihydrochloride \| Theophylline \| Acefylline \| Curcumin \| Theophylline monohydrate \| Sodium 4-phenylbutyrate \| Vorinostat \| Parthenolide

阿贝司他|||PCI-24781|||PCI24781|||PCI 24781|||CRA 24781|||CRA 024781|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