Fimepinostat (CUDC-907)

中文名称:非美诺司他

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

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
5mg RMB 975.24 现货
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客户使用Selleck的Fimepinostat (CUDC-907)发表文献34

产品质控

批次: 纯度: 99.97%
99.95

Fimepinostat (CUDC-907)相关产品

相关信号通路图

HDAC抑制剂选择性比较

细胞实验数据示例

细胞系 实验类型 给药浓度 孵育时间 活性描述 文献信息
MV4-11 Antiproliferative assay 25 to 50 nM 72 hrs Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability at 25 to 50 nM after 72 hrs by tryphan blue assay 32212730
human Glioma cells (HF2476) Cytotoxicity assay 72 h Cytotoxicity against human Glioma cells (HF2476) after 72 hrs by CelltiterGlo assay, EC50=0.7 nM 26288699
human Glioma cells (HF2790)  Cytotoxicity assay 72 h Cytotoxicity against human Glioma cells (HF2790) after 72 hrs by CelltiterGlo assay, EC50=0.7 nM 26288699
human Glioma cells (HF2876)  Cytotoxicity assay 72 h Cytotoxicity against human Glioma cells (HF2876) after 72 hrs by CelltiterGlo assay, EC50=0.7 nM 26288699
human Glioma cells (HF3013) Cytotoxicity assay 72 h Cytotoxicity against human Glioma cells (HF3013) after 72 hrs by CelltiterGlo assay, EC50=0.7 nM 26288699
human Glioma cells (HF2885) Cytotoxicity assay 72 h Cytotoxicity against human Glioma cells (HF2885) after 72 hrs by CelltiterGlo assay, EC50=0.7 nM 26288699
human Glioma cells (HF2381) Cytotoxicity assay 72 h Cytotoxicity against human Glioma cells (HF2381) after 72 hrs by CelltiterGlo assay, EC50=0.7 nM 26288699
human Glioma cells (HF2303) Cytotoxicity assay 72 h Cytotoxicity against human Glioma cells (HF2303) after 72 hrs by CelltiterGlo assay, EC50=0.7 nM 26288699
MV4-11 Cytotoxicity assay 24 hrs Cytotoxicity against human MV4-11 cells assessed as growth inhibition after 24 hrs by MTT assay, =0.00043μM. 27186676
Sf9 Function assay 15 mins Inhibition of full length C-terminal His-tagged human recombinant HDAC3/NCOR2 (395 to 489 residues) expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substr, =0.0018μM. 27186676
Sf9 Function assay 15 mins Inhibition of human recombinant HDAC10 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence assay, =0.0028μM. 27186676
Sf9 Function assay 15 mins Inhibition of full length human recombinant HDAC2 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence a, =0.005μM. 27186676
Sf9 Function assay 15 mins Inhibition of full length human recombinant HDAC11 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence , =0.0054μM. 27186676
A2780S Cytotoxicity assay 24 hrs Cytotoxicity against human A2780S cells assessed as growth inhibition after 24 hrs by MTT assay, =0.00615μM. 27186676
HCT116 Cytotoxicity assay 24 hrs Cytotoxicity against human HCT116 cells assessed as growth inhibition after 24 hrs by MTT assay, =0.00734μM. 27186676
Sf9 Function assay 60 mins Inhibition of full length recombinant human N-terminal GST-tagged p110 alpha/untagged p85 alpha expressed in baculovirus infected insect Sf9 cells using PI:3PS as substrate incubated for 60 mins by ADP-Glo luminescence assay, =0.019μM. 27186676
Sf9 Function assay 15 mins Inhibition of full length human recombinant HDAC6 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence a, =0.027μM. 27186676
Sf9 Function assay 2 hrs Inhibition of N-terminal His6-tagged recombinant full-length human p110delta/untagged recombinant full length human p85alpha expressed in baculovirus infected insect Sf9 cells incubated for 2 hrs by kinase-glo assay, =0.039μM. 27186676
Sf9 Function assay 1 hr Inhibition of recombinant human p110beta expressed in baculovirus infected insect Sf9 cells incubated for 1 hr by ADP-gloreagen assay, =0.054μM. 27186676
A2780S Function assay 6 hrs Inhibition of HDAC1/2/3 in human A2780S cells assessed as histone H3 acetylation incubated for 6 hrs by cytoblot assay, =0.12625μM. 27186676
Sf9 Function assay 15 mins Inhibition of full length C-terminal His-tagged human recombinant HDAC8 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after , =0.191μM. 27186676
A2780S Function assay 6 hrs Inhibition of HDAC6 in human A2780S cells assessed as tubulin acetylation incubated for 6 hrs by cytoblot assay, =0.22175μM. 27186676
Sf9 Function assay 15 mins Inhibition of N-terminal GST/C-terminal His-tagged human recombinant HDAC4 (627 to 1084 residues) expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrat, =0.409μM. 27186676
Sf9 Function assay 15 mins Inhibition of N-terminal GST-tagged human recombinant HDAC7 (518 to end residues) expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measu, =0.426μM. 27186676
Sf9 Function assay 15 mins Inhibition of C-terminal His-tagged human recombinant HDAC9 (604 to 1066 residues) expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition meas, =0.554μM. 27186676
Sf9 Function assay 15 mins Inhibition of human recombinant HDAC5 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence assay, =0.674μM. 27186676
Sf9 Function assay 15 mins Inhibition of recombinant C-terminal His/FLAG-tagged HDAC1 (unknown origin) expressed in baculovirus infected Sf9 insect cells using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr, =0.00036μM. 31117517
Sf9 Function assay 15 mins Inhibition of recombinant human full length C-terminal His-tagged HDAC8 expressed in baculovirus infected Sf9 insect cells using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr, =0.0014μM. 31117517
Sf9 Function assay 15 mins Inhibition of recombinant human full length HDAC2 expressed in baculovirus infected Sf9 insect cells using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr, =0.0016μM. 31117517
HCT116 Antiproliferative assay 96 hrs Antiproliferative activity against human HCT116 cells after 96 hrs by MTT assay, =0.005μM. 31117517
HCT8 Antiproliferative assay 96 hrs Antiproliferative activity against human HCT8 cells after 96 hrs by MTT assay, =0.005μM. 31117517
U87 Antiproliferative assay 96 hrs Antiproliferative activity against human U87 cells after 96 hrs by MTT assay, =0.007μM. 31117517
Capan2 Antiproliferative assay 96 hrs Antiproliferative activity against human Capan2 cells after 96 hrs by MTT assay, =0.007μM. 31117517
MDA-MB-453 Antiproliferative assay 96 hrs Antiproliferative activity against human MDA-MB-453 cells after 96 hrs by MTT assay, =0.009μM. 31117517
Bel7402 Antiproliferative assay 96 hrs Antiproliferative activity against human Bel7402 cells after 96 hrs by MTT assay, =0.013μM. 31117517
HepG2 Antiproliferative assay 96 hrs Antiproliferative activity against human HepG2 cells after 96 hrs by MTT assay, =0.015μM. 31117517
NCI-H1299 Antiproliferative assay 96 hrs Antiproliferative activity against human NCI-H1299 cells after 96 hrs by MTT assay, =0.025μM. 31117517
MCF7 Antiproliferative assay 96 hrs Antiproliferative activity against human MCF7 cells after 96 hrs by MTT assay, =0.041μM. 31117517
HGC27 Antiproliferative assay 96 hrs Antiproliferative activity against human HGC27 cells after 96 hrs by MTT assay, =0.041μM. 31117517
Sf9 Function assay 15 mins Inhibition of recombinant human full length HDAC11 expressed in baculovirus infected Sf9 insect cells using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr, =0.132μM. 31117517
NCI-H460 Antiproliferative assay 96 hrs Antiproliferative activity against human NCI-H460 cells after 96 hrs by MTT assay, =0.15μM. 31117517
SW1990 Antiproliferative assay 96 hrs Antiproliferative activity against human SW1990 cells after 96 hrs by MTT assay, =0.18μM. 31117517
K562 Antiproliferative assay 96 hrs Antiproliferative activity against human K562 cells after 96 hrs by MTT assay, =0.28μM. 31117517
Sf9 Function assay 15 mins Inhibition of recombinant human full length HDAC4 expressed in baculovirus infected Sf9 insect cells using Ac-peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr, =0.445μM. 31117517
DU145 Antiproliferative assay 96 hrs Antiproliferative activity against human DU145 cells after 96 hrs by MTT assay, =0.56μM. 31117517
HuH7 Antiproliferative assay 96 hrs Antiproliferative activity against human HuH7 cells after 96 hrs by MTT assay, =0.56μM. 31117517
Sf9 Function assay Inhibition of recombinant full length human N-terminal GST-tagged PI3K p110alpha/untagged p85alpha expressed in baculovirus infected insect Sf9 cells by ADP-Glo luminescent assay, =0.019μM. 28494256
Sf9 Function assay Inhibition of recombinant full length human N-terminal GST-tagged PI3K p110delta/untagged p85alpha expressed in baculovirus infected insect Sf9 cells by ADP-Glo luminescent assay, =0.039μM. 28494256
Sf9 Function assay Inhibition of recombinant full length human N-terminal GST-tagged PI3K p110beta/untagged p85alpha expressed in baculovirus infected insect Sf9 cells by ADP-Glo luminescent assay, =0.054μM. 28494256
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells 29435139
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
U-2 OS qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells 29435139
Rh30 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells 29435139
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells 29435139
U-2 OS qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells 29435139
Rh30 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for SK-N-SH cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for SJ-GBM2 cells 29435139
Daoy qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for Daoy cells 29435139
Sf9 Function assay Inhibition of recombinant human full-length N-terminal GST-tagged p110alpha/untagged full-length p85alpha expressed in baculovirus infected Sf9 cells using PIP2 as substrate by ADP-glo luminescence assay, =0.019μM. 30418766
Sf9 Function assay Inhibition of recombinant human full-length N-terminal GST-tagged p110delta/untagged full-length p85alpha expressed in baculovirus infected Sf9 cells using PIP2 as substrate by ADP-glo luminescence assay, =0.039μM. 30418766
Sf9 Function assay Inhibition of recombinant human full-length N-terminal GST-tagged p110beta/untagged full-length p85alpha expressed in baculovirus infected Sf9 cells using PIP2 as substrate by ADP-glo luminescence assay, =0.054μM. 30418766
点击查看更多细胞系数据

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(In Vitro)
体外研究活性

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]

实验图片 检测方法 检测指标 实验图片 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
Immunofluorescence γ-H2AX / 53BP1 RAD51 29760046
Growth inhibition assay Cell viability 28147336
体内研究(In Vivo)
体内研究活性

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]

动物实验 Animal Models 携带NHL和 MM模型的小鼠
Dosages 100 mg/kg
Administration 口服处理
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02909777 Active not recruiting
Lymphoma|Neuroblastoma|Brain Tumor|Solid Tumor
Dana-Farber Cancer Institute|Curis Inc.
October 2016 Phase 1
NCT02307240 Completed
Triple-Negative Breast Cancer|High-grade Serous Ovarian Cancer|Solid Tumors|NUT Midline Carcinoma
Curis Inc.
November 2014 Phase 1
NCT01742988 Completed
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

化学信息&溶解度

分子量 508.55 分子式

C23H24N8O4S

CAS号 1339928-25-4 SDF Download Fimepinostat (CUDC-907) SDF
Smiles CN(CC1=CC2=C(S1)C(=NC(=N2)C3=CN=C(C=C3)OC)N4CCOCC4)C5=NC=C(C=N5)C(=O)NO
储存条件(自收到货起)

体外溶解度
批次:

DMSO : 100 mg/mL ( 196.63 mM; DMSO吸湿会降低化合物溶解度,请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩尔浓度计算器

体内溶解度
批次:

现配现用,请按从左到右的顺序依次添加,澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量 浓度 体积 分子量

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。

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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.

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