Fimepinostat (CUDC-907)

For research use only. Not for use in humans.

目录号:S2759 中文名称:非美诺司他

Fimepinostat (CUDC-907) Chemical Structure

CAS No. 1339928-25-4

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。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 4500.71 现货
RMB 2207.14 现货
RMB 8763.3 现货
RMB 20229.3 现货
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客户使用Selleck生产的Fimepinostat (CUDC-907)发表文献28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 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)
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) M3\HSGN6fG:2b4jpZ4l1gSCjc4PhfS=> MVS3NkBp MmTCR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gS4xqd22jIHPlcIx{KCiKRkK4PFUqKGGodHXyJFczKGi{czDifUBE\WyudHn0[ZJIdG9iYYPzZZktKEWFNUC9NE44KG6P NHr3S|k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkK4PFY6QSd-Mk[yPFg3QTl:L3G+
human Glioma cells (HF3013) M4nzRWN6fG:2b4jpZ4l1gSCjc4PhfS=> NUjzclNzPzJiaB?= NW\N[mtRS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hT2yrb33hJINmdGy|IDjISlMxOTNrIHHmeIVzKDd{IHjyd{BjgSCFZXzseIl1\XKJbH:gZZN{[XluIFXDOVA:OC55IH7N MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjJ6OE[5PUc,OjZ{OEi2PVk9N2F-
human Glioma cells (HF2876)  Ml\zR5l1d3SxeHnjbZR6KGG|c3H5 MnnvO|IhcA>? MX;DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDHcIlwdWFiY3XscJMhMEiIMki3Okkh[W[2ZYKgO|IhcHK|IHL5JGNmdGy2aYTldmdtdyCjc4PhfUwhTUN3ME2wMlchdk1? NX7VfHFURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[yPFg3QTlpPkK2Nlg5Pjl7PD;hQi=>
human Glioma cells (HF2790)  MnnWR5l1d3SxeHnjbZR6KGG|c3H5 NETDVm44OiCq M33tS2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGdtcW:vYTDj[YxteyBqSF[yO|kxMSCjZoTldkA4OiCqcoOgZpkhS2WubITpeIVzT2yxIHHzd4F6NCCHQ{WwQVAvPyCwTR?= NWntU3V7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[yPFg3QTlpPkK2Nlg5Pjl7PD;hQi=>
human Glioma cells (HF2476) M17IeGN6fG:2b4jpZ4l1gSCjc4PhfS=> NFTs[JI4OiCq NV35[XR{S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hT2yrb33hJINmdGy|IDjISlI1PzZrIHHmeIVzKDd{IHjyd{BjgSCFZXzseIl1\XKJbH:gZZN{[XluIFXDOVA:OC55IH7N M4W0XFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4Mki4Olk6Lz5{NkK4PFY6QTxxYU6=
human Glioma cells (HF2381) NH3sXYtEgXSxdH;4bYNqfHliYYPzZZk> MVq3NkBp MorkR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gS4xqd22jIHPlcIx{KCiKRkKzPFEqKGGodHXyJFczKGi{czDifUBE\WyudHn0[ZJIdG9iYYPzZZktKEWFNUC9NE44KG6P M1fwUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4Mki4Olk6Lz5{NkK4PFY6QTxxYU6=
human Glioma cells (HF2303) M3qyU2N6fG:2b4jpZ4l1gSCjc4PhfS=> MUi3NkBp M{nPTWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGdtcW:vYTDj[YxteyBqSF[yN|A{MSCjZoTldkA4OiCqcoOgZpkhS2WubITpeIVzT2yxIHHzd4F6NCCHQ{WwQVAvPyCwTR?= NHPMenA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkK4PFY6QSd-Mk[yPFg3QTl:L3G+
MV4-11 MXzDfZRwfG:6aXPpeJkh[XO|YYm= MnvxNlQhcHK| MVPDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNWlQuOTFiY3XscJMh[XO|ZYPz[YQh[XNiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhOjRiaILzJIJ6KE2WVDDhd5NigSxiPUCuNFAxPDQQvF2u NEHZWXc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{G4OlY4Pid-MkexPFY3PzZ:L3G+
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Sf9 NVXyXXRGTnWwY4Tpc44h[XO|YYm= NY[x[IdvOTVibXnudy=> MmnVTY5pcWKrdHnvckBw\iCodXzsJIxmdme2aDDoeY1idiC{ZXPvcYJqdmGwdDDISGFEOTFiZYjwdoV{e2WmIHnuJIJi[3Wub4\pdpV{KGmwZnXjeIVlKGmwc3XjeEBU\jliY3XscJMhfXOrbnegRYMueGWydHnk[U1CVUNiYYOgd5Vje3S{YYTlJIF{e2W|c3XkJIF{KHKnbHXhd4Uhd2ZiQV3DJJBz\WmwY4XiZZRm\CCob4KgNVUhdWmwczDmc4xtd3enZDDifUB{fWK|dILheIUh[WSmaYTpc44hdWWjc4Xy[YQh[W[2ZYKgNUBpeiCkeTDmcJVwemW|Y3XuZ4UhNCB;MD6wNFU1|ryPLh?= NFj2bZo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{G4OlY4Pid-MkexPFY3PzZ:L3G+
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HCT116 Mo[xR5l1d3SxeHnjbZR6KGG|c3H5 MVGyOEBpenN? NF\kfWxEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJS1RzMU[gZ4VtdHNiYYPz[ZN{\WRiYYOg[5Jwf3SqIHnubIljcXSrb36gZYZ1\XJiMkSgbJJ{KGK7IF3UWEBie3OjeTygQVAvODB5M{VOwG0v NWTnW29tRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkexPFY3PzZpPkK3NVg3Pjd4PD;hQi=>
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K562 NWCwVZZNSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= M1[yUFk3KGi{cx?= MmfqRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCNNU[yJINmdGy|IHHmeIVzKDl4IHjyd{BjgSCPVGSgZZN{[XluIE2wMlI5|ryPLh?= NGPlSZQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MUGxO|UyPyd-M{GxNVc2OTd:L3G+
Sf9 Mmn6SpVv[3Srb36gZZN{[Xl? NH\BcIYyPSCvaX7z NE\yZ3pKdmirYnn0bY9vKG:oIILlZ49u[mmwYX70JIh2dWGwIH\1cIwhdGWwZ4ToJGhFSUN2IHX4dJJme3OnZDDpckBj[WO3bH;2bZJ2eyCrbn\lZ5Rm\CCVZkmgbY5{\WO2IHPlcIx{KHW|aX7nJGFkNXCncITp[IUh[XNic4Xid5Rz[XSnIIDy[Ylv[3WkYYTl[EBnd3JiMUWgcYlveyCob3zsc5dm\CCkeTDzeYJ{fHKjdHWgZYRlcXSrb36gZY5lKG2nYYP1doVlKGGodHXyJFEhcHJuIE2wMlQ1Pc7:TT6= NFTBTpE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MUGxO|UyPyd-M{GxNVc2OTd:L3G+
DU145 NGTXRXJCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NEG3U5k6PiCqcoO= NIfYNmJCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFTVNVQ2KGOnbHzzJIFnfGW{IEm2JIhzeyCkeTDNWHQh[XO|YYmsJF0xNjV4zszNMi=> MoHKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzFzMUe1NVcoRjNzMUG3OVE4RC:jPh?=
HuH7 MVXBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NWXsXIZqQTZiaILz MmHVRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKdVi3JINmdGy|IHHmeIVzKDl4IHjyd{BjgSCPVGSgZZN{[XluIE2wMlU3|ryPLh?= MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{OTFzN{WxO{c,OzFzMUe1NVc9N2F-
MV4-11 NHHDXZVCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= MX6yOUB1dyB3MDDuUS=> M{jnRVczKGi{cx?= MUHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2YND2xNUBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iY3XscEB3cWGkaXzpeJkh[XRiMkWgeI8hPTBibl2gZYZ1\XJiN{KgbJJ{KGK7IITyfZBp[W5iYnz1[UBie3OjeR?= MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{OjJzMkezNEc,OzJ{MUK3N|A9N2F-

... Click to View More Cell Line Experimental Data

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; 

PubMed: 30353642     


Western blots showing protein expression in lysates of MEC-1 cells treated with CUDC-907 at various concentrations or DMSO as a control (0) for 12 h. AKT, p-AKT (Ser473), p-p70S6K (Thr389), Ac-H3K9, ERK, p-ERK (Thr202/Tyr204), p-MEK (Ser217/221), STAT3, p-STAT3 (Tyr705), MCL-1, BCL-2, BCL-xL, and PARP were detected with specific antibodies. β-actin was used as a loading control. 

p-PRAS40 / p-4EBP1 / p-S6 / c-Myc / Cleaved PARP / Caspase-3 / Celaved caspase-3 ; 

PubMed: 28147336     


Western blot analysis demonstrating the effect of increasing concentration of CUDC-907 (from 0.01 to 1 μM) on PI3K downstream targets (p4EBP1, pPRAS40 and pS6) and histone H3 acetylation (Ac Histone H3). The actual inhibition of PI3K and HDAC resulted in a decrease in c-Myc protein levels. Activation of caspase 3 and PARP was present as well. 

SYK / BTK / Bcl-10 / MyD88 / IRAK4 ; 

PubMed: 28147336     


Western blot confirming the effect of CUDC-907 (0.1 μM for 24 hours) on BCR and TLR signaling proteins in B-cell lymphoma cell lines (GCB n = 3 and ABC n = 3).

30353642 28147336
Immunofluorescence
γ-H2AX / 53BP1; 

PubMed: 29760046     


Representative images and quantification of immunofluorescence staining for γH2AX and 53BP1 in SF188 cells treated with radiotherapy (4 Gy), CUDC-907 (100 nmol/L), or combination treatment in which radiotherapy was combined with KU70 siRNA, RAD51 siRNA (48 hours after siRNA transfection), or CUDC-907 (16 hours prior to 4 Gy).

RAD51; 

PubMed: 29760046     


Representative images and quantification of immunofluorescence staining for γH2AX and RAD51 in SF188 cells treated with radiotherapy (4 Gy), CUDC-907 (100 nmol/L), or combination treatment in which radiotherapy was combined with KU70 siRNA, RAD51 siRNA (48 hours after siRNA transfection), or CUDC-907 (16 hours prior to 4 Gy).

29760046
Growth inhibition assay
Cell viability; 

PubMed: 28147336     


MTS assay of 8 representative DLBCL and 2 Hodgkin lymphoma cell lines treated with increasing dose of CUDC-907 from 0.01 to 10 μM for 24, 48, 72 hours. Error bars represent standard error of the mean (S.E.M) of triplicate experiments. 

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]

- 合并
  • Animal Models: 携带NHL和 MM模型的小鼠
  • Dosages: 100 mg/kg
  • Administration: 口服处理
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 102 mg/mL (200.57 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 508.55
化学式

C23H24N8O4S

CAS号 1339928-25-4
储存条件 粉状
溶于溶剂
别名 N/A

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
NCT02909777 Recruiting Drug: CUDC-907 Lymphoma|Neuroblastoma|Brain Tumor|Solid Tumor Dana-Farber Cancer Institute|Curis Inc. October 2016 Phase 1
NCT02674750 Completed Drug: CUDC-907 Relapsed and/or Refractory Diffuse Large B-cell Lymphoma Including With Myc Alterations Curis Inc. January 2016 Phase 2
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

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

如果有其他问题,请给我们留言。

  • * 必填项

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.

HDAC Signaling Pathway Map

HDAC Inhibitors with Unique Features

相关HDAC产品

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID