Fimepinostat (CUDC-907)

目录号:S2759 中文名称:非美诺司他

仅限科研使用

CUDC-907是一种PI3K和HDAC双重抑制剂,作用于PI3KαHDAC1/2/3/10IC50分别为19 nM和1.7 nM/5 nM/1.8 nM/2.8 nM。CUDC-907 在乳腺癌细胞中可诱导细胞周期阻滞与凋亡。Phase 1。

Fimepinostat (CUDC-907) Chemical Structure

CAS: 1339928-25-4

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 811.3 现货
RMB 975.24 现货
大包装 有超大折扣

今日订购,明日送达 全国免运费 分装免费 分装成小规格产品(单支最小为1mg)
如1支10mg产品可分装为10支1mg产品

全国免费电话:400-668-6834   |   Email:info@selleck.cn

客户使用Selleck生产的Fimepinostat (CUDC-907)发表文献29篇:

产品安全说明书

HDAC抑制剂选择性比较

相关HDAC产品

生物活性

产品描述 CUDC-907是一种PI3K和HDAC双重抑制剂,作用于PI3KαHDAC1/2/3/10IC50分别为19 nM和1.7 nM/5 nM/1.8 nM/2.8 nM。CUDC-907 在乳腺癌细胞中可诱导细胞周期阻滞与凋亡。Phase 1。
靶点
HDAC1 [1]
(Cell-free assay)
HDAC3 [1]
(Cell-free assay)
HDAC10 [1]
(Cell-free assay)
HDAC2 [1]
(Cell-free assay)
HDAC11 [1]
(Cell-free assay)
点击更多
1.7 nM 1.8 nM 2.8 nM 5.0 nM 5.4 nM
体外研究

PI3K/HDAC Inhibitor 抑制其他PI3K亚型,如 PI3Kβ, PI3Kγ, PI3Kδ和 PI3KɑE545K , IC50 分别为 54, 311, 39 和62 nM。而且, PI3K/HDAC Inhibitor 也抑制HDAC亚型HDAC8, HDAC6 和 HDAC11,IC50分别为191, 27 和 5.4 nM。此外, PI3K/HDAC Inhibitor 低效抑制其他类型 HDAC 酶活性。PI3K/HDAC Inhibitor 抑制一系列B细胞淋巴瘤生长,如Granta 519, DOHH2, RL, Pfeiffer, SuDHL4, Daudi 和 Raji,IC50 分别为 7, 1, 2, 4, 3, 15 和 9 nM。PI3K/HDAC Inhibitor 也阻断 骨髓瘤增殖,如RPMI8226, OPM-2 和 ARH77,IC50分别为 2, 1 和5 nM。PI3K/HDAC Inhibitor 作用于多发性骨髓瘤和B细胞淋巴瘤,具有有效抗癌活性。[1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human Glioma cells (HF2885) MXjDfZRwfG:6aXPpeJkh[XO|YYm= MnnPO|IhcA>? MoW3R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gS4xqd22jIHPlcIx{KCiKRkK4PFUqKGGodHXyJFczKGi{czDifUBE\WyudHn0[ZJIdG9iYYPzZZktKEWFNUC9NE44KG6P NUPPZZhTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[yPFg3QTlpPkK2Nlg5Pjl7PD;hQi=>
human Glioma cells (HF3013) MXzDfZRwfG:6aXPpeJkh[XO|YYm= NIfEWlk4OiCq NIrpZ|NEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBIdGmxbXGgZ4VtdHNiKFjGN|AyOyliYX\0[ZIhPzJiaILzJIJ6KEOnbHz0bZRmekeubzDhd5NigSxiRVO1NF0xNjdibl2= NXvpPZlpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[yPFg3QTlpPkK2Nlg5Pjl7PD;hQi=>
human Glioma cells (HF2876)  NVHmTIhOS3m2b4TvfIlkcXS7IHHzd4F6 NEXzPG84OiCq MYPDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDHcIlwdWFiY3XscJMhMEiIMki3Okkh[W[2ZYKgO|IhcHK|IHL5JGNmdGy2aYTldmdtdyCjc4PhfUwhTUN3ME2wMlchdk1? NI\IS3g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkK4PFY6QSd-Mk[yPFg3QTl:L3G+
human Glioma cells (HF2790)  M4LuU2N6fG:2b4jpZ4l1gSCjc4PhfS=> NU\DZWdQPzJiaB?= NUf3bpl4S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hT2yrb33hJINmdGy|IDjISlI4QTBrIHHmeIVzKDd{IHjyd{BjgSCFZXzseIl1\XKJbH:gZZN{[XluIFXDOVA:OC55IH7N M4HjTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4Mki4Olk6Lz5{NkK4PFY6QTxxYU6=
human Glioma cells (HF2476) NFTa[otEgXSxdH;4bYNqfHliYYPzZZk> MXO3NkBp M4XCXGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGdtcW:vYTDj[YxteyBqSF[yOFc3MSCjZoTldkA4OiCqcoOgZpkhS2WubITpeIVzT2yxIHHzd4F6NCCHQ{WwQVAvPyCwTR?= MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjJ6OE[5PUc,OjZ{OEi2PVk9N2F-
human Glioma cells (HF2381) M1naemN6fG:2b4jpZ4l1gSCjc4PhfS=> NX7HRnVnPzJiaB?= MYfDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDHcIlwdWFiY3XscJMhMEiIMkO4NUkh[W[2ZYKgO|IhcHK|IHL5JGNmdGy2aYTldmdtdyCjc4PhfUwhTUN3ME2wMlchdk1? MlrjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ{OEi2PVkoRjJ4Mki4Olk6RC:jPh?=
human Glioma cells (HF2303) NYHO[IxYS3m2b4TvfIlkcXS7IHHzd4F6 NFvTV4E4OiCq NVP5S204S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hT2yrb33hJINmdGy|IDjISlI{ODNrIHHmeIVzKDd{IHjyd{BjgSCFZXzseIl1\XKJbH:gZZN{[XluIFXDOVA:OC55IH7N NXLESIlIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[yPFg3QTlpPkK2Nlg5Pjl7PD;hQi=>
MV4-11 NY\WXWk4S3m2b4TvfIlkcXS7IHHzd4F6 NF[0fmEzPCCqcoO= MUTDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNWlQuOTFiY3XscJMh[XO|ZYPz[YQh[XNiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhOjRiaILzJIJ6KE2WVDDhd5NigSxiPUCuNFAxPDQQvF2u NGDlV209[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{G4OlY4Pid-MkexPFY3PzZ:L3G+
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Assay
Methods Test Index PMID
Western blot AKT / p-AKT / P-p70S6K1 / Ac-H3K9 / p-MEK / p-ERK / p-STAT3 / MCL-1 / Bcl-2 / Bcl-xl / PARP p-PRAS40 / p-4EBP1 / p-S6 / c-Myc / Cleaved PARP / Caspase-3 / Celaved caspase-3 SYK / BTK / Bcl-10 / MyD88 / IRAK4 30353642 28147336
Immunofluorescence γ-H2AX / 53BP1 RAD51 29760046
Growth inhibition assay Cell viability 28147336
体内研究 PI3K/HDAC Inhibitor 口服给药犬类具有生物有效性。PI3K/HDAC Inhibitor 治疗小鼠肿瘤具有长的半衰期。PI3K/HDAC Inhibitor 作用于移植瘤,诱导凋亡,且抑制癌细胞增殖。在高效性研究中, PI3K/HDAC Inhibitor 按最大耐受剂量(MTD)处理,作用于NHL和MM模型,比单独药剂PI3K或HDAC抑制剂参考化合物或两者联用更有效。而且, PI3K/HDAC Inhibitor 按MTD剂量处理,比PI3Kδ选择性抑制剂CAL-101更有效。[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)

动物实验:

[1]

  • Animal Models: 携带NHL和 MM模型的小鼠
  • Dosages: 100 mg/kg
  • Administration: 口服处理

溶解度(25°C)

体外

* 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 508.55
化学式

C23H24N8O4S

CAS号 1339928-25-4
储存条件 3年 -20°C 粉状
2年 -80°C 溶于溶剂

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)

mg/kg g μL

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,: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: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: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。

摩尔浓度计算器

质量 浓度 体积 分子量

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02909777 Recruiting Drug: CUDC-907 Lymphoma|Neuroblastoma|Brain Tumor|Solid Tumor Dana-Farber Cancer Institute|Curis Inc. October 2016 Phase 1
NCT02307240 Completed Drug: CUDC-907 Triple-Negative Breast Cancer|High-grade Serous Ovarian Cancer|Solid Tumors|NUT Midline Carcinoma Curis Inc. November 2014 Phase 1
NCT01742988 Completed Drug: fimepinostat|Drug: Rituximab|Drug: venetoclax Lymphoma|Relapsed Lymphoma|Refractory Lymphoma|Relapsed and/or Refractory Lymphoma|Relapsed Ddiffuse Large B-Cell Lymphoma (DLBCL)|Refractory Diffuse Large B-Cell Lymphoma (DLBCL)|Relapsed and/or Refractory Diffuse Large B-Cell Lymphoma (DLBCL)|Double-hit Lymphoma (DHL)|Triple-hit Lymphoma (THL)|Double-expressor Lymphoma (DEL)|High-grade B-cell Lymphoma (HGBL) Curis Inc.|The Leukemia and Lymphoma Society December 2012 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

技术支持

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操作手册

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常见问题及建议解决方法

问题 1:
How to solve CUDC-907 for in vivo studies (p.o.)?

回答:
If you decided to take P.O. as your administration route, we suggest you to use 1% CMC-Na to dilute CUDC-907 as a suspension solution for gavage.

问题 2:
What is the half-life of CUDC-907 in vivo?

回答:
GUDC-907 is said to have a long half-life in mouse tumor model: http://cancerres.aacrjournals.org/content/72/8_Supplement/3744.short, however, its not formally published and we have no detail of how long it is.