Abexinostat (PCI-24781)

For research use only. Not for use in humans.

目录号:S1090 别名: CRA-024781

Abexinostat (PCI-24781) Chemical Structure

CAS No. 783355-60-2

Abexinostat (PCI-24781, CRA-024781) 是一种新型的pan-HDAC抑制剂,靶向作用于HDAC1Ki为7 nM,对HDACs 2, 3, 6,和10有适中的抑制性,但比作用于HDAC8选择性强40倍。Phase 1/2。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 2217.61 现货
RMB 1406.39 现货
RMB 2628.91 现货
RMB 7938.64 现货
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客户使用Selleck生产的Abexinostat (PCI-24781)发表文献20篇:

产品安全说明书

HDAC抑制剂选择性比较

生物活性

产品描述 Abexinostat (PCI-24781, CRA-024781) 是一种新型的pan-HDAC抑制剂,靶向作用于HDAC1Ki为7 nM,对HDACs 2, 3, 6,和10有适中的抑制性,但比作用于HDAC8选择性强40倍。Phase 1/2。
靶点
HDAC1 [1]
(Cell-free assay)
HDAC3/SMRT [1] HDAC6 [1] HDAC2 [1]
(Cell-free assay)
HDAC10 [1]
7 nM(Ki) 8.2 nM(Ki) 17 nM(Ki) 19 nM(Ki) 24 nM
体外研究

PCI-24781针对于多种肿瘤细胞系具有有效的抗肿瘤活性,GI50分布于0.15 μM 到3.09 μM之间。PCI-24781也抑制HUVEC 内皮细胞的增值,GI50为0.43 μM。PCI-24781处理导致HCT116 和 DLD-1细胞系中组蛋白乙酰化和微管蛋白乙酰化的剂量依赖性积累,同时诱导p21表达,PARP的剪切以及γH2AX的累积[1]。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。与抑制HR 一致,在CHO细胞中,PCI-24781处理后导致I-SceI诱导染色质断裂引起的同源定向修复能力下降[2]。PCI-24781诱发S 期缺失,G2期细胞周期停滞以及软组织(STS)细胞的凋亡。PCI-24781诱导STS细胞中Rad51 的转录抑制很有可能是通过增强E2F1在Rad51近端启动子区域的结合[3]。PCI-24781也诱导Hodgkin淋巴瘤和非霍奇金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[4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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MG 63 (6-TG R) MoXudWhVWyCjc4PhfS=> NWLOR3ZoeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhVUdiNkOgLFYuXEdiUjmgZ4VtdHN? Mnj2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
U-2 OS NHj3e4pyUFSVIHHzd4F6 MULxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDVMVIhV1NiY3XscJM> NEHDb3k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
Rh41 M2\HSZFJXFNiYYPzZZk> NIH2VGZyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBTcDRzIHPlcIx{ NWTVSoZ3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
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OHS-50 Ml;ndWhVWyCjc4PhfS=> M3;sdJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJG9JWy13MDDj[Yxtew>? M1PjeVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
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... Click to View More Cell Line Experimental Data

体内研究 PCI-24781按200 mg/kg 剂量作用于移植小鼠,隔一天一次,明显抑制HCT116 和 DLD-1肿瘤细胞生长,抑制效果分别是69%和59%。PCI-24781按20 mg/kg, 40 mg/kg, 80 mg/kg和160 mg/kg剂量每星期连续四天给药处理,然后三天不给药处理((一天一次,每周四天))作用于HCT116移植小鼠模型,抑制效果分别是48%, 57%, 82.2%, 和80.0%[1]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:[1]
- 合并

HDAC 酶活鉴定:

运用连续胰蛋白酶耦合分析法检测HDAC酶活。将100μL反应体系置于96孔板中分析抑制剂表征。将HDAC 酶添加到50 mM HEPES, 100 mM KCl, 0.001% Tween 20, 5% DMSO (pH 7.4) 以及补充了牛血清蛋白 (BSA)的反应体系中,与不同浓度的PCI-24781混合均匀,孵育15分钟。每种HDAC同工酶使用的BSA浓度不一样,分别是0% (HDAC1),0.01% (HDAC2, 3, 8, 10)和0.05% (HDAC6)。胰蛋白酶的终浓度是50 nM,acetyl-Gly-Ala-(N-acetyl-Lys)-AMC的终浓度是25μM(HDAC1,HDAC3,HDAC6),50μM (HDAC2,HDAC10)和100 μM (HDAC8),起始反应。设置八个复孔的阴性对照中不加入PCI-24781。使用酶标仪检测反应。经过30分钟的延迟时间,通过355纳米的激发波和460纳米吸收波得到荧光值。检测反应速率是测定增强荧光所需的反应时间。使用程序BatchKi可以得到抑制常数K i (app)
细胞实验:[1]
- 合并
  • Cell lines: HCT116, HCT-15, BT-549, NCI-H226, CWR-22RV1, MCF-7, NCI-PC3, DLD-1, SKOV-3和 OVCAR-3细胞
  • Concentrations: 0–10 μM,溶于 DMSO
  • Incubation Time: 48, 72, 96和120 小时
  • Method: 运用一种微量蓝色荧光的细胞增殖试验检测PCI-24781处理后细胞增殖,细胞至少培养两倍增。细胞接种于96孔板,PCI-24781设置9个从0.0015 μM 到10 μM半对数不等间隔的浓度梯度,每一梯度设计三个复孔。DMSO终浓度每孔0.15%。设定抑制细胞增殖GI50在达到50% 到 95%之间为置信区间,运用四参数方程,利用非线性回归曲线计算PCI-24781的有效浓度。
    (Only for Reference)
动物实验:[1]
- 合并
  • Animal Models: 携带HCT116 和DLD-1移植瘤细胞的BALB/c nu/nu 雌小鼠
  • Dosages: ~200 mg/kg
  • Administration: 每隔一天一次或者每星期连续四天,停滞三天。
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 80 mg/mL (201.29 mM)
Water Insoluble
Ethanol Insoluble

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 397.42
化学式

C21H23N3O5

CAS号 783355-60-2
储存条件 粉状
溶于溶剂
别名 CRA-024781

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 ul 动物数量
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
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03934567 Recruiting Drug: Abexinostat Lymphoma Follicular Xynomic Pharmaceuticals Inc. April 22 2020 Phase 2
NCT03939182 Recruiting Drug: Abexinostat|Drug: Ibrutinib Diffuse Large B-cell Lymphoma|Mantle Cell Lymphoma Memorial Sloan Kettering Cancer Center|Janssen Scientific Affairs LLC|Xynomic Pharmaceuticals Inc. May 29 2019 Phase 1|Phase 2
NCT03600441 Active not recruiting Drug: Abexinostat Follicular Lymphoma Xynomic Pharmaceuticals Inc. August 27 2018 Phase 2
NCT01543763 Recruiting Drug: PZP115891 PCI-24781 Metastatic Solid Tumors Pamela Munster|Pharmacyclics LLC.|Novartis|Xynomic Pharmaceuticals Inc.|GlaxoSmithKline Research and Education Foundation for Cardiovascular Disease|University of California San Francisco June 25 2012 Phase 1
NCT01027910 Completed Drug: PCI-24781|Drug: Doxorubicin|Drug: GCSF Sarcoma Massachusetts General Hospital|Dana-Farber Cancer Institute|Brigham and Women''s Hospital|Pharmacyclics LLC. February 2009 Phase 1|Phase 2

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID