Domatinostat (4SC-202)

For research use only. Not for use in humans.

目录号:S7555

Domatinostat (4SC-202) Chemical Structure

CAS No. 910462-43-0

Domatinostat (4SC-202)是一种选择性的I类HDAC抑制剂,对HDAC1,HDAC2,和HDAC3的IC50分别为1.20 μM,1.12 μM,和0.57 μM。也对Lysine specific demethylase 1 (LSD1)表现出抑制活性。Phase 1。

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产品安全说明书

HDAC抑制剂选择性比较

生物活性

产品描述 Domatinostat (4SC-202)是一种选择性的I类HDAC抑制剂,对HDAC1,HDAC2,和HDAC3的IC50分别为1.20 μM,1.12 μM,和0.57 μM。也对Lysine specific demethylase 1 (LSD1)表现出抑制活性。Phase 1。
靶点
HDAC3 [1]
(Cell-free assay)
HDAC2 [1]
(Cell-free assay)
HDAC1 [1]
(Cell-free assay)
HDAC11 [1]
(Cell-free assay)
HDAC5 [1]
(Cell-free assay)
0.57 μM 1.12 μM 1.20 μM 9.7 μM 11.3 μM
体外研究

在HeLa细胞中,4SC-202诱导组蛋白H3高度乙酰化,EC50 为1.1 μM。4SC-202通过干扰有丝分裂纺锤体的正常发育诱导G2/M细胞周期阻滞,并引起纺锤体塌陷和多个成核中心。此外,4SC-202对人癌症细胞系表现出广谱抗肿瘤活性,IC50 为0.7 μM。[1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
CRL-2105 NWfLcZZXS2WubDD2bYFjcWyrdImgZZN{[Xl? MkHxO|LjiImq Mly1TWM2OD1zN{Cgcm0> M{e5dlMxQDh3MkWw
MyLa M3O1cmNmdGxidnnhZoltcXS7IHHzd4F6 M1\MSVcz6oDLaB?= MYTJR|UxRTF7MDDuUS=> M1T6OVMxQDh3MkWw
CRL-8294 NHi3cINE\WyuII\pZYJqdGm2eTDhd5NigQ>? NULCdZg3PzMkgJno NFjRfnJKSzVyPUK2NEBvVQ>? MmHEN|A5QDV{NUC=
HTB-176 NUTlPFl1S2WubDD2bYFjcWyrdImgZZN{[Xl? NVXoW405PzMkgJno MmewTWM2OD1|N{Cgcm0> MnnrN|A5QDV{NUC=
Se-Ax Mm\OR4VtdCC4aXHibYxqfHliYYPzZZk> NHHkNIs4OuLCiXi= NG\IVlJKSzVyPUK1NEBvVQ>? Ml;KN|A5QDV{NUC=
HuT 78 MoDDR4VtdCC4aXHibYxqfHliYYPzZZk> NEXOeFc4OuLCiXi= MVzJR|UxRTN|MDDuUS=> M4T1cFMxQDh3MkWw

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
Ac α-tubulin / Ac Histone H3 / Ac Histone H4 ; 

PubMed: 27250763     


Levels of acetylated α-tubulin and histone H3 and H4 were quantified in VM-CUB1 and UM-UC-3 cells after defined 4SC-202 treatment (0.5/2.5 μM, 24/48 h). Treatment with 3 nM romidepsin served as positive control for H3 and H4 acetylation; treatment with 2.5 μM SAHA served as a positive control for acetylated α-tubulin. DMSO was the solvent control.

Cyclin A / Cyclin B1 / Cyclin D1 / Cyclin E / p21 ; 

PubMed: 27250763     


Cyclins (A, B1, D1, E) and p21 protein expression levels following 4SC-202 (0.5/2.5 μM) or 2.5 μM SAHA treatment were quantified by western blot analysis in comparison to DMSO treatment in VM-CUB1 and UM-UC-3 cells (24/48 h)

Caspase-3 / Cleaved Caspase-3 / H3K4me2 / H3K9ac ; 

PubMed: 30885250     


Total cell lysates harvested after 48 h of drug treatment were subjected to immunoblot analysis using antibodies recognizing the indicated targets (H3K4me2: histone H3 dimethyl lysine 4; H3K9ac: histone H3 acetyl lysine 9)

27250763 30885250
Growth inhibition assay
Cell viability ; 

PubMed: 27250763     


UCCs and control cells were treated with increasing amounts of the class I HDAC specific inhibitor 4SC-202. The dose–response curves after 72 h 4SC-202 treatment are shown exemplarily for the UCCs VM-CUB1 and UM-UC-3 and the non-urothelial control cells HBLAK and HEK-293.

IC50; 

PubMed: 30885250     


IC50 doses for 4SC-202 and FK228-treated cells were calculated by nonlinear fitting of the MTS data

27250763 30885250
体内研究 在体内,4SC-202具有较高的口服生物利用度,并表现出高代谢稳定性和低血浆清除率。在A549 NSCLC 异种移植和RKO27结肠癌模型中,4SC-202 (120 mg/kg p.o.)表现出显著的强抗肿瘤活性。[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)

细胞实验:

[1]

- 合并
  • Cell lines: NCI-H460,A549,MCF7,MDA-MB-468,SK-BR-3,SK-OV-3,A2780,RKO (p21),HCT-15,PC-3,HeLa,Cal 27,A-431,Hec-1-A,K-562,EOL1,和 CCRF-CEM 细胞
  • Concentrations: ~10 μM
  • Incubation Time: 72小时
  • Method:

    CRC cell lines (HT-29, HCT-116, HCT-15, and DLD1), the primary human colon cancer cells, or primary human colon epithelial cells were treated with applied concentrations of 4SC-202, cells were further cultured for indicated time, and cell survival was tested by MTT assay or trypan blue staining assay; cell proliferation was tested by clonogenicity assay. Expression of listed proteins was tested by Western blots.


    (Only for Reference)
动物实验:

[1]

- 合并
  • Animal Models: A549 NSCLC 移植瘤模型和 RKO27 结肠癌模型
  • Dosages: 120 mg/kg
  • Administration: p.o.
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 89 mg/mL (198.87 mM)
Water Insoluble
Ethanol Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
10mg/mL

* 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 447.51
化学式

C23H21N5O3S

CAS号 910462-43-0
储存条件 粉状
溶于溶剂
别名

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、MSDS / 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、MSDS / 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
NCT01344707 Completed Drug: 4SC-202 Advanced Hematologic Malignancies 4SC AG March 2011 Phase 1

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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:

    Do you have suggestions about the in vivo formulation of the compound?

  • 回答:

    For in vivo study, we recommend to use 2% DMSO+30% PEG 300+5% Tween 80+ddH2O with solubility up to 10mg/ml.

HDAC Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID