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Rac-Belinostat

Rac-Belinostat

产品编号 T1852   CAS 414864-00-9
别名: NSC726630, PXD101, PX-105684

Rac-Belinostat (PX-105684) 是一种具有抗肿瘤活性的新型异羟肟酸型组蛋白脱乙酰酶 (HDAC) 抑制剂。 Belinostat 靶向 HDAC 酶,从而抑制肿瘤细胞增殖、诱导细胞凋亡、促进细胞分化和抑制血管生成。这种药物可以使耐药肿瘤细胞对其他抗肿瘤药物敏感,可能是通过一种涉及胸苷酸合酶下调的机制。

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Rac-Belinostat Chemical Structure
Rac-Belinostat, CAS 414864-00-9
规格 价格/CNY 货期 数量
1 mg ¥ 198 现货
5 mg ¥ 393 现货
10 mg ¥ 647 现货
25 mg ¥ 1,050 现货
50 mg ¥ 1,490 现货
100 mg ¥ 2,190 现货
200 mg ¥ 3,490 现货
500 mg ¥ 5,580 现货
1 mL * 10 mM (in DMSO) ¥ 513 现货
其他形式的 Rac-Belinostat:
产品目录号及名称: Rac-Belinostat (T1852)
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纯度: 99.96%
纯度: 99.93%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 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.
靶点活性 HDAC:27 nM
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。
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.
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)
别名 NSC726630, PXD101, PX-105684
化合物与蛋白结合的复合物

T1852_1

Crystal structure of Danio rerio histone deacetylase 6 catalytic domain 2 in complex with belinostat

分子量 318.35
分子式 C15H14N2O4S
CAS No. 414864-00-9

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 60 mg/mL (188.5 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.1412 mL 15.706 mL 31.412 mL 78.5299 mL
5 mM 0.6282 mL 3.1412 mL 6.2824 mL 15.706 mL
10 mM 0.3141 mL 1.5706 mL 3.1412 mL 7.853 mL
20 mM 0.1571 mL 0.7853 mL 1.5706 mL 3.9265 mL
50 mM 0.0628 mL 0.3141 mL 0.6282 mL 1.5706 mL
100 mM 0.0314 mL 0.1571 mL 0.3141 mL 0.7853 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Plumb JA, et al. Mol Cancer Ther, 2003, 2(8), 721-728. 2. Buckley MT, et al. J Transl Med, 2007, 5:49. 3. Qian X, et al. Mol Cancer Ther, 2006, 5(8), 2086-2095. 4. Chowdhury S, et al. J Biol Chem, 2011, 286(35), 30937-30948. 5. Duan J, et al. Mol Cancer Ther, 2007, 6(1), 37-50. 6. Zuo Y, Xu H, Chen Z, et al. 17‑AAG synergizes with Belinostat to exhibit a negative effect on the proliferation and invasion of MDA‑MB‑231 breast cancer cells[J]. Oncology Reports. 2020, 43(6): 1928-1944.

文献引用

1. Zuo Y, Xu H, Chen Z, et al. 17‑AAG synergizes with Belinostat to exhibit a negative effect on the proliferation and invasion of MDA‑MB‑231 breast cancer cells. Oncology Reports. 2020, 43(6): 1928-1944. 2. Wang C, Huang M, Lin Y, et al.ENO2-derived phosphoenolpyruvate functions as an endogenous inhibitor of HDAC1 and confers resistance to antiangiogenic therapy.Nature Metabolism.2023: 1-22.
ITF3756 AR42 CHDI-390576 Nexturastat A Resminostat hydrochloride HDAC-IN-40 NSC 3852 Crebinostat

相关化合物库

该产品包含在如下化合物库中:
抗癌活性化合物库 抗癌药物库 抗癌上市药物库 抗癌临床化合物库 NO PAINS 化合物库 抗癌化合物库 上市药物库 NF-κB 通路分子库 经典已知活性库 已知活性化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
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% ddH2O
计算 重置

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Rac-Belinostat 414864-00-9 Chromatin/Epigenetic DNA Damage/DNA Repair HDAC NSC 726630 NSC726630 NSC-726630 Belinostat PX 105684 PX105684 PXD101 PXD 101 PX-105684 PXD-101 Inhibitor inhibitor inhibit

 

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