Ricolinostat (ACY-1215)

别名: Rocilinostat

Ricolinostat (ACY-1215, Rocilinostat) 是一种选择性HDAC6抑制剂,无细胞试验中IC50为5 nM,作用于HDAC6比作用于HDAC1/2/3(I型HDACs)选择性高10倍以上,对HDAC8具有微弱的作用活性,对HDAC4/5/7/9/11, Sirtuin1和Sirtuin2具有最小的作用活性。Ricolinostat (ACY-1215) 可抑制细胞增殖并促进凋亡。Phase 2。

Ricolinostat (ACY-1215)  Chemical Structure

Ricolinostat (ACY-1215) Chemical Structure

CAS: 1316214-52-4

规格 价格 库存 购买数量
10mM (1mL in DMSO) 1170 现货
5mg 900.21 现货
50mg 4664.38 现货
1g 10401.3 现货
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常与Ricolinostat (ACY-1215) 一起在实验中被使用的化合物

Bendamustine


与单独使用任一药物相比,Ricolinostat和Bendamustine在淋巴瘤细胞系中诱导显着更大的细胞凋亡。

Cosenza M, et al. Apoptosis. 2017 Jun;22(6):827-840.

Carfilzomib (PR-171)


Ricolinostat和Carfilzomib显着抑制MCL异种移植模型中的肿瘤生长。

Dasmahapatra G, et al. Mol Cancer Ther (2014) 13 (12): 2886–2897.

Crizotinib


Ricolinostat和Crizotinib治疗显着抑制DLBCL细胞的细胞生长,并诱导NuDUL-1和Toledo细胞凋亡。

Liu Z, et al. J Pathol. 2018 Oct;246(2):141-153.

Oxaliplatin


Ricolinostat增强Oxaliplatin在结直肠癌细胞中的抗癌活性。

Lee DH, et al. Int J Oncol. 2018 Aug;53(2):844-854.

(+)-JQ1


Ricolinostat和JQ1增加细胞凋亡,减少c-MYC和BCL-2的表达,并降低多发性骨髓瘤细胞增殖。

Carew JS, et al. Blood Adv. 2019 Apr 23;3(8):1318-1329.

Ricolinostat (ACY-1215) 相关产品

相关信号通路图

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
SUP-B15 Function assay 0.1 to 10 uM 24 hrs Inhibition of HDAC6 in imatinib-resistant human SUP-B15 cells assessed as increase in cleaved PARP expression at 0.1 to 10 uM after 24 hrs by immunoblot assay 30365892
SEM Function assay 0.1 to 10 uM 24 hrs Inhibition of HDAC6 in human SEM cells assessed as increase in cleaved PARP expression at 0.1 to 10 uM after 24 hrs by immunoblot assay 30365892
HL60 Function assay 0.1 to 10 uM 24 hrs Inhibition of HDAC6 in human HL60 cells assessed as increase in cleaved PARP expression at 0.1 to 10 uM after 24 hrs by immunoblot assay 30365892
SUP-B15 Function assay 0.1 to 10 uM 24 hrs Inhibition of HDAC6 in imatinib-resistant human SUP-B15 cells assessed as increase in acetyl-histone H3 expression at 0.1 to 10 uM after 24 hrs by immunoblot assay 30365892
SEM Function assay 0.1 to 10 uM 24 hrs Inhibition of HDAC6 in human SEM cells assessed as increase in acetyl-histone H3 expression at 0.1 to 10 uM after 24 hrs by immunoblot assay 30365892
HL60 Function assay 0.1 to 10 uM 24 hrs Inhibition of HDAC6 in human HL60 cells assessed as increase in acetyl-histone H3 expression at 0.1 to 10 uM after 24 hrs by immunoblot assay 30365892
SUP-B15 Function assay 0.1 to 10 uM 24 hrs Inhibition of HDAC6 in imatinib-resistant human SUP-B15 cells assessed as increase in acetyl-alpha tubulin expression at 0.1 to 10 uM after 24 hrs by immunoblot assay 30365892
SEM Function assay 0.1 to 10 uM 24 hrs Inhibition of HDAC6 in human SEM cells assessed as increase in acetyl-alpha tubulin expression at 0.1 to 10 uM after 24 hrs by immunoblot assay 30365892
HL60 Function assay 0.1 to 10 uM 24 hrs Inhibition of HDAC6 in human HL60 cells assessed as increase in acetyl-alpha tubulin expression at 0.1 to 10 uM after 24 hrs by immunoblot assay 30365892
MV4-11 Function assay 1000 nM 6 hrs Inhibition of HDAC1/2/3 in human MV4-11 cells assessed as upregulation of histone H3 acetylation at 1000 nM after 6 hrs by Western blot analysis 26443078
OPM2 Cell Viability Assay 0-8μM 48 h decreases MM-cell viability in a dose-dependent manner 22262760
MM.1R Cell Viability Assay 0-8μM 48 h decreases MM-cell viability in a dose-dependent manner 22262760
LR5 Cell Viability Assay 0-8μM 48 h decreases MM-cell viability in a dose-dependent manner 22262760
RPMI Cell Viability Assay 0-8μM 48 h decreases MM-cell viability in a dose-dependent manner 22262760
OPM1 Cell Viability Assay 0-8μM 48 h decreases MM-cell viability in a dose-dependent manner 22262760
MM.1S Cell Viability Assay 0-8μM 48 h decreases MM-cell viability in a dose-dependent manner 22262760
RPMI8226  Function Assay 0.25/1μM 18 h increases acetylated α-tubulin 22262760
MM.1S Function Assay 0.25/1μM 18 h increases acetylated α-tubulin 22262760
MM.1R Function Assay 0.25/1μM 18 h increases acetylated α-tubulin 22262760
MM.1S Function Assay 0-5μM 6 h increases acetylated α-tubulin 22262760
A-172 Growth Inhibition Assay 10 nM 24/48 h inhibits cell growth time dependently 26150340
U87MG Growth Inhibition Assay 10 nM 24/48 h inhibits cell growth time dependently 26150340
HEL Cell cycle assay 1 to 10 uM 48 hrs Cell cycle arrest in human HEL cells assessed as accumulation at G1 phase at 1 to 10 uM after 48 hrs propidium iodide staining based flow cytometry 29940115
SEM Function assay 1.6 uM 18 hrs Inhibition of HDAC6 in human SEM cells assessed as decrease in aggresome accumulation at 1.6 uM after 18 hrs by FACS analysis 30365892
SH-SY5Y Function assay 0.1 to 1 uM 24 hrs Inhibition of HDAC6 in human SH-SY5Y cells assessed as increase in acetylation of alpha-tubulin at 0.1 to 1 uM after 24 hrs by Western blot analysis 30028616
SH-SY5Y Function assay 0.1 to 1 uM 24 hrs Inhibition of class 1 HDAC in human SH-SY5Y cells assessed as increase in acetylation of histone H3 at 0.1 to 1 uM after 24 hrs by Western blot analysis 30028616
BCP-ALL Cytotoxicity assay 72 hrs Cytotoxicity against human BCP-ALL cells derived from patient 3 after 72 hrs by CellTiter-Glo luminescent cell viability assay, IC50 = 4.45 μM. 30365892
HEL Antiproliferative assay 48 hrs Antiproliferative activity against human HEL cells after 48 hrs by CCK-8 assay, IC50 = 3.75 μM. 29940115
K562 Antiproliferative assay 48 hrs Antiproliferative activity against human K562 cells after 48 hrs by CCK-8 assay, IC50 = 3.75 μM. 29940115
HL60 Antiproliferative assay 48 hrs Antiproliferative activity against human HL60 cells after 48 hrs by CCK-8 assay, IC50 = 3.75 μM. 29940115
KCL22 Cytotoxicity assay 72 hrs Cytotoxicity against human KCL22 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay, IC50 = 3.75 μM. 30365892
SUP-B15 Cytotoxicity assay 72 hrs Cytotoxicity against imatinib-resistant human SUP-B15 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay, IC50 = 3.54 μM. 30365892
U266 Cytotoxicity assay 72 hrs Cytotoxicity against human U266 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay, IC50 = 3.52 μM. 30365892
KCL22 Cytotoxicity assay 72 hrs Cytotoxicity against imatinib-resistant human KCL22 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay, IC50 = 3.38 μM. 30365892
HEL Antiproliferative assay 48 hrs Antiproliferative activity against human HEL cells after 48 hrs in presence of JAK2 inhibitor CYT-387 by CCK-8 assay, IC50 = 2.54 μM. 29940115
K562 Antiproliferative assay 48 hrs Antiproliferative activity against human K562 cells after 48 hrs in presence of JAK2 inhibitor CYT-387 by CCK-8 assay, IC50 = 2.54 μM. 29940115
HL60 Antiproliferative assay 48 hrs Antiproliferative activity against human HL60 cells after 48 hrs in presence of JAK2 inhibitor CYT-387 by CCK-8 assay, IC50 = 2.54 μM. 29940115
HL60 Cytotoxicity assay 72 hrs Cytotoxicity against human HL60 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay, IC50 = 2.36 μM. 30365892
RPMI18226 Cytotoxicity assay 72 hrs Cytotoxicity against human RPMI18226 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay, IC50 = 1.97 μM. 30365892
SUP-B15 Cytotoxicity assay 72 hrs Cytotoxicity against human SUP-B15 cells after 72 hrs by CellTiter-Glo luminescent cell viability assay, IC50 = 1.92 μM. 30365892
SEM Cytotoxicity assay 72 hrs Cytotoxicity against human SEM cells after 72 hrs by CellTiter-Glo luminescent cell viability assay, IC50 = 1.61 μM. 30365892
RPMI8226 Cytotoxicity assay 72 hrs Cytotoxicity against human RPMI8226 cells after 72 hrs by MTT assay, IC50 = 1.468 μM. 26443078
BCP-ALL Cytotoxicity assay 72 hrs Cytotoxicity against human BCP-ALL cells derived from patient 2 after 72 hrs by CellTiter-Glo luminescent cell viability assay, IC50 = 0.58 μM. 30365892
BCP-ALL Cytotoxicity assay 72 hrs Cytotoxicity against human BCP-ALL cells derived from patient 4 after 72 hrs by CellTiter-Glo luminescent cell viability assay, IC50 = 0.54 μM. 30365892
BCP-ALL Cytotoxicity assay 72 hrs Cytotoxicity against human BCP-ALL cells derived from patient 1 after 72 hrs by CellTiter-Glo luminescent cell viability assay, IC50 = 0.29 μM. 30365892
Sf9 Function assay 15 mins Inhibition of full length recombinant human C-terminal FLAG/His-tagged HDAC1 expressed in baculovirus infected sf9 cells using Boc-Lys-(Ac)-AMC as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence ass, IC50 = 0.1 μM. 29500130
Sf9 Function assay 15 mins Inhibition of full length recombinant human C-terminal His-tagged HDAC2 expressed in baculovirus infected sf9 cells using Boc-Lys-(Ac)-AMC as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence assay, IC50 = 0.066 μM. 29500130
Sf9 Function assay 10 mins Inhibition of full length human recombinant C-terminal FLAG-His-tagged HDAC1 expressed in Sf9 cells using FTS as substrate preincubated for 10 mins followed by substrate addition measured over 30 mins, IC50 = 0.058 μM. 28038324
Sf9 Function assay 10 mins Inhibition of full length human recombinant C-terminal FLAG-tagged HDAC2 expressed in Sf9 cells using FTS as substrate preincubated for 10 mins followed by substrate addition measured over 30 mins, IC50 = 0.048 μM. 28038324
Sf9 Function assay 15 mins Inhibition of full length recombinant human C-terminal His-tagged HDAC3/N-terminal GST-tagged NCOR2 (395 to 489 residues) expressed in baculovirus infected sf9 cells using Boc-Lys-(Ac)-AMC as substrate preincubated for 15 mins followed by substrate additi, IC50 = 0.037 μM. 29500130
Sf9 Function assay 15 mins Inhibition of full length recombinant human N-terminal GST-tagged HDAC6 expressed in baculovirus infected sf9 cells using Boc-Lys-(Ac)-AMC as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence assay, IC50 = 0.009 μM. 29500130
Sf9 Function assay 10 mins Inhibition of full length human recombinant N-terminal GST-tagged HDAC6 expressed in Sf9 cells using FTS as substrate preincubated for 10 mins followed by substrate addition measured over 30 mins, IC50 = 0.0047 μM. 28038324
HH Growth Inhibition Assay 48 h IC50=2.5 μM 26116270
Sup-T1 Growth Inhibition Assay 48 h IC50=1.6 μM 26116270
CCL-119 Growth Inhibition Assay 48 h IC50=1.7 μM 26116270
H9 Growth Inhibition Assay 48 h IC50=1.2 μM 26116270
Rec-1  Growth Inhibition Assay 48 h IC50=2.3 μM 26116270
Jeko-1 Growth Inhibition Assay 48 h IC50=1.5 μM 26116270
Jvm-2 Growth Inhibition Assay 48 h IC50=4.0 μM 26116270
Su-DHL6 Growth Inhibition Assay 48 h IC50=3.2 μM 26116270
Hbl-2 Growth Inhibition Assay 48 h IC50=1.9 μM 26116270
Su-DHL4 Growth Inhibition Assay 48 h IC50=4.7 μM 26116270
OCI-Ly1 Growth Inhibition Assay 48 h IC50=2.4 μM 26116270
OCI-Ly7 Growth Inhibition Assay 48 h IC50=1.2 μM 26116270
Su-DHL2 Growth Inhibition Assay 48 h IC50=3.3 μM 26116270
OCI-Ly10 Growth Inhibition Assay 48 h IC50=0.9 μM 26116270
Riva Growth Inhibition Assay 48 h IC50=2.2 μM 26116270
Hbl-1 Growth Inhibition Assay 48 h IC50=1.6 μM 26116270
SEM Antiproliferative assay 24 to 72 hrs Antiproliferative activity against human SEM cells at IC50 to 2 times IC50 after 24 to 72 hrs by trypan exclusion method 30365892
SEM Function assay 18 hrs Inhibition of HDAC6 in human SEM cells assessed as decrease in aggresome accumulation at IC50 after 18 hrs by fluorescence microscopic method 30365892
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells 29435139
Rh30 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 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
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD 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
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 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
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 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
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 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
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
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 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
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells 29435139
点击查看更多细胞系数据

生物活性

产品描述 Ricolinostat (ACY-1215, Rocilinostat) 是一种选择性HDAC6抑制剂,无细胞试验中IC50为5 nM,作用于HDAC6比作用于HDAC1/2/3(I型HDACs)选择性高10倍以上,对HDAC8具有微弱的作用活性,对HDAC4/5/7/9/11, Sirtuin1和Sirtuin2具有最小的作用活性。Ricolinostat (ACY-1215) 可抑制细胞增殖并促进凋亡。Phase 2。
特性 ACY-1215作用于4名健康捐献者的PHA刺激的PBMCs,与pan-HDAC抑制剂SAHA相比,具有更低的细胞毒性。
靶点
HDAC6 [1]
(Cell-free assay)
HDAC2 [1]
(Cell-free assay)
HDAC3 [1]
(Cell-free assay)
HDAC1 [1]
(Cell-free assay)
HDAC8 [1]
(Cell-free assay)
4.7 nM 48 nM 51 nM 58 nM 100 nM
体外研究(In Vitro)
体外研究活性

ACY-1215是一种异羟肟酸类衍生物。ACY-1215作用于HDAC1, HDAC2, 和 HDAC3 (I型 HDACs)效果分别低12,10, 和 11倍。ACY-1215最低活性作用于(IC50>1μM) HDAC4, HDAC5, HDAC7, HDAC9, HDAC11, Sirtuin1,和 Sirtuin2,对HDAC8(IC50=0.1μM)具有轻微的作用活性。ACY-1215作用于T细胞毒性的IC50值为2.5μM。ACY-1215作用于骨髓(BM)环境,克服BMSCs和细胞因子赋予的肿瘤细胞生长和存活。

实验图片 检测方法 检测指标 实验图片 PMID
Western blot Ac-α-tubulin / Ac-Histone H4 Survivin / P21 / CDC2 / p53 / p-p53(S392) / Cyclin A2 / Cyclin B1 Bax / Bim / Bcl2 / Cleaved caspase-3 / Cleaved caspase-9 / Cleaved PARP PI3K(p85) / AKT / p-AKT(S473) / PRAS40 / Rag C / mTOR / p-mTOR / ERK / p-ERK Ac-β-catenin(K49) / p-β-catenin / β-catenin 31015208
Immunofluorescence β-tubulin / β-catenin 25546293
Growth inhibition assay Cell viability 31015208
体内研究(In Vivo)
体内研究活性

。比单独使用具有更显著的抗MM 活性。ACY-1215易被肿瘤组织吸收。此外,药物不会在肿瘤组织中累积,处理24小时后,血液细胞和肿瘤组织的乙酰化的α-tubulin平行下降。[1]

动物实验 Animal Models MM移植瘤SCID小鼠模型
Dosages 50 mg/kg
Administration 腹腔注射
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02632071 Completed
Metastatic Breast Cancer|Breast Carcinoma
Columbia University|Acetylon Pharmaceuticals Incorporated|National Cancer Institute (NCI)
March 1 2016 Phase 1
NCT01583283 Completed
Multiple Myeloma
Celgene
July 12 2012 Phase 1
NCT01323751 Completed
Multiple Myeloma
Celgene|The Leukemia and Lymphoma Society
July 2011 Phase 1|Phase 2

化学信息&溶解度

分子量 433.5 分子式

C24H27N5O3

CAS号 1316214-52-4 SDF Download Ricolinostat (ACY-1215) SDF
Smiles C1=CC=C(C=C1)N(C2=CC=CC=C2)C3=NC=C(C=N3)C(=O)NCCCCCCC(=O)NO
储存条件(自收到货起)

体外溶解度
批次:

DMSO : 42 mg/mL ( (96.88 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:
What would you suggest to obtain a clear solution?

回答:
S8001 ACY-1215 can be dissolved in 2% DMSO/30% PEG 300/ddH2O at 5 mg/ml clearly while it in 1% DMSO/30% polyethylene glycol/1% Tween 80 at 30 mg/ml is a suspension for oral administration. Please note that the precipitation will go out from the clear solution after stayed for about half an hour, So it is recommended to prepare the solution just before use.

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