基本信息 产品详情 公司简介 推荐产品
  • 首页
  • 个人中心
  • 委托采购
  • 采购清单
网站主页 化工产品目录 生物化工 抑制剂 表观遗传学(Epigenetics) HDAC 抑制剂 贝利司他(PXD101) 化合物 Belinostat
  • 化合物 Belinostat|T1852|TargetMol

化合物 Belinostat|T1852|TargetMol

Rac-Belinostat
414864-00-9
￥119 1mg 起订
￥236 5mg 起订
￥388 10mg 起订
上海 更新日期：2024-09-23

TargetMol中国（陶术生物）

VIP12年
联系人：邵小姐
电话：021-021-33632979拨打
手机：15002134094 拨打
邮箱：marketing@targetmol.com

产品详情:

中文名称：
化合物 Belinostat
英文名称：
Rac-Belinostat
CAS号：
414864-00-9
品牌：
TargetMol
产地：
美国
保存条件：
Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
纯度规格：
99.96%
产品类别：
抑制剂
货号：
T1852

Product Introduction

Bioactivity

名称Rac-Belinostat
描述Rac-Belinostat (PX-105684) is a novel hydroxamic acid-type histone deacetylase (HDAC) inhibitor with antineoplastic activity. Belinostat targets HDAC enzymes, thereby inhibiting tumor cell proliferation, inducing apoptosis, promoting cellular differentiation, and inhibiting angiogenesis. This agent may sensitize drug-resistant tumor cells to other antineoplastic agents, possibly through a mechanism involving the down-regulation of thymidylate synthase.
细胞实验Tumor cell lines are seeded in 5 mL of medium at a density of 8 × 104 cells/25 cm2 flask and incubated for 48 hours. Cells are exposed to Belinostat (0.016 to 10 μM) for 24 hours. The medium is removed, and 1 mL of trypsin/EDTA is added to each flask. Once the cells have detached, 1 mL of medium is added, the cells are resuspended, and those from the control untreated flask are counted. Cells are diluted and plated into 6-cm Petri dishes (three per flask) at a density of 0.5-2× 103 cells/dish depending on the cell line. Cells from the drug-treated flasks are diluted and plated as for the control flasks. Dishes are incubated for 10–15 days at 37 °C. Cells are washed with PBS, fixed in methanol, and stained with crystal violet, and colonies that contained ≥50 cells counted. Sensitivity is expressed as the IC50 defined as the concentration of belinostat required to reduce the number of colonies to 50% of that of the control untreated cells.(Only for Reference)
激酶实验Histone Deacetylase Activity: Subconfluent cultures are harvested and washed twice in ice cold PBS and pelleted by centrifugation at 200 × g for 5 min. The cell pellet is resuspended in two volumes of lysis buffer [60 mM Tris buffer (pH 7.4) containing 30% glycerol and 450 mM NaCl] and lysed by three freeze (dry ice) thaw (30 °C water bath) cycles. Cell debris is removed by centrifugation at 1.2 × 104 g for 5 min, and the supernatant is stored at ?80 °C. Histone H4 peptide (sequence SGRGKGGKGLGKGGAKRHRK corresponding to the 20 NH2-terminal residues) is acetylated by a recombinant protein containing the hypoxanthine-aminopterin-thymidine domain of p300, using [3H]acetyl CoA as a source of acetate. H4 peptide (100 μg) is mixed with hypoxanthine-aminopterin-thymidine buffer (50 mM Tris HCl pH 8.0, 5% glycerol, 50 mM KCl, and 0.1 mM EDTA), 1 mM DTT, 1 mM 4-(2-aminoethyl) benzenesulfonylfluoride, 1 × complete protease inhibitors, 50 μL of purified p300, and 1.85 m [3H]acetyl CoA (4.50Ci/mmol) in a final volume of 300 μL and incubated at 30 °C for 45 min. The p300 protein is removed by incubation with 20 μL of 50% Ni-agaroase beads for 1 hour at 4 °C and centrifugation. The supernatant is applied to a 2 mL Sephadex G15 column, and the flow through is collected. One milliliter of distilled Water is gently applied, and three drop fractions are collected; this is repeated until 4–5 mL of distilled Water has been added, and ～40 fractions are collected. Three microliters of each fraction are diluted in 2 mL of scintillation fluid and counted in a scintillation counter to identify the fractions containing the labeled peptide. These fractions are pooled, and 1 μL of the combined sample is measured to assess the radioactivity in every peptide batch (3-7×103 cpm/μL). For activity assays, the reaction is carried out in a total volume of 150 μL of buffer [60 mM Tris (pH 7.4) containing 30% glycerol] containing 2 μL of cell extract and, where used, 2 μL of belinostat.The reaction is started by the addition of 2 μL of [3H] labeled substrate (acetylated histone H4 peptide corresponding to the 20 NH2-terminal residues). Samples are incubated at 37 °C for 45 min, and the reaction stopped by the addition of HCl and acetic acid (0.72 and 0.12 M final concentrations, respectively). Released [3H]acetate is extracted into 750 μL of ethyl acetate, and samples are centrifuged at 1.2× 104 g for 5 min. The upper phase (600 μL) is transferred to 3 mL of scintillation fluid and counted.
体外活性在鼠膀胱细胞中,Belinostat诱导p21WAF1, HDAC 核心和细胞通讯基因.在A2780和A2780/cp70 移植瘤中,Belinostat（10 mg/kg）可明显延迟肿瘤生长,但不影响动物体重.Belinostat（100 mg/kg）单独处理A2780移植瘤,可使肿瘤抑制率达47% ,该作用存在剂量依赖性.Belinostat（100 mg/kg）和Carboplatin（40 mg/kg）联用可在18.6-22.5 天延迟肿瘤生长时.此外,作用于携带抗Bortezomib UMSCC-11A移植瘤的鼠时,该化合物显示肠胃毒性.硼替佐米与Belinostat联用对肿瘤显著抑制效果.
体内活性Belinostat 对A2780/cp70 和2780AD细胞的活性很低, 这两个细胞由抗阿霉素及顺铂的A2780细胞衍生。在卵巢癌细胞系中,Belinostat可增强微管乙酰化。 Belinostat对肿瘤细胞生长(包括A2780, HCT116, HT29, WIL, CALU-3, MCF7, PC3,及HS852)有抑制作用（IC50：0.2-0.66 μM）。通过组蛋白H3/H4乙酰化和PARP分裂,Belinostat可诱导细胞凋亡。 Belinostat抑制膀胱癌细胞尤其是5637细胞的生长,细胞在G0-G1期积累, 在S期下降,在 G2-M期上升。 Belinostat对细胞生长活性的抑制作用与多重耐药表现型无关,但是多西他赛的活性明显受影响。Belinostat 可增强卡铂或多西他赛对A2780和OVCAR-3细胞活性的抑制。在TGF-β信号依赖机制中,Belinostat使蛋白激酶A激活并使survivin mRNA降低。
存储条件Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度Ethanol : < 1 mg/mL (insoluble or slightly soluble)
H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 65 mg/mL (204.18 mM)
关键字NSC 726630 | NSC-726630 | Belinostat | PX 105684 | Rac-Belinostat | PX105684 | PXD 101 | PXD-101
相关产品Valproic acid sodium salt | 4-Phenylbutyric acid | Valproic Acid | Panobinostat | Methyl L-histidinate dihydrochloride | Theophylline | Acefylline | Curcumin | Theophylline monohydrate | Sodium 4-phenylbutyrate | Vorinostat | Parthenolide
相关库抑制剂库 | 经典已知活性库 | 抗癌活性化合物库 | 抗癌上市药物库 | 已知活性化合物库 | 抗衰老化合物库 | FDA 上市药物库 | 药物功能重定位化合物库 | 抗癌临床化合物库 | 抗癌药物库
PXD101|||PX-105684|||NSC726630|TargetMol

公司简介

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。 从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。 经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期 (12年)
注册资本 566.2651万人民币
员工人数 100-500人
年营业额 ￥ 1亿以上
经营模式 贸易,试剂,定制,服务
主营行业 化学试剂,生物活性小分子

化合物 Belinostat相关厂家报价

  • 414864-00-9
  • 414864-00-9
  • 成都彼样生物科技有限公司 VIP
  • 2024-11-28
  • 询价
内容声明
official 进入官方账号
拨打电话 立即询价