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Panobinostat

Panobinostat

产品编号 T2383   CAS 404950-80-7
别名: 帕比司他, NVP-LBH589, LBH589

Panobinostat (NVP-LBH589) 是一种广谱的 HDAC 抑制剂 (IC50=5 nM),具有口服活性和非选择性。Panobinostat 具有抗肿瘤活性,可以诱导细胞凋亡自噬

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Panobinostat Chemical Structure
Panobinostat, CAS 404950-80-7
规格 价格/CNY 货期 数量
1 mg ¥ 153 现货
5 mg ¥ 335 现货
10 mg ¥ 526 现货
25 mg ¥ 933 现货
50 mg ¥ 1,530 现货
100 mg ¥ 2,570 现货
200 mg ¥ 3,820 现货
500 mg ¥ 6,220 现货
1 mL * 10 mM (in DMSO) ¥ 375 现货
其他形式的 Panobinostat:
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
Venetoclax限时半价
产品目录号及名称: Panobinostat (T2383)
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选择批次  
纯度: 99.14%
纯度: 99.01%
纯度: 99.01%
纯度: 97.2%
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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 Panobinostat (NVP-LBH589) is a broad-spectrum HDAC inhibitor (IC50=5 nM) with oral activity and non-selectivity. Panobinostat has antitumor activity and induces apoptosis and autophagy.
靶点活性 HDAC (MOLT-4 cells):5 nM, HDAC (Reh cells):20 nM
体外活性 方法:37 种肺癌细胞系用 Panobinostat (0-800 nmol/L) 处理 48-72 h,使用 MTT 方法检测细胞活力。
结果:Panobinostat 对人和小鼠的肺癌细胞系表现出强大的抗增殖活性和细胞毒性。[1]
方法:人 ALL 细胞 MOLT-4 和 Reh 用 Panobinostat (10-100 nM) 处理 24-72 h,使用 Flow Cytometry 检测细胞凋亡情况。
结果:Panobinostat 以时间和剂量依赖的方式诱导 MOLT-4 和 Reh 细胞的凋亡。[2]
体内活性 方法:为检测体内抗肿瘤活性,将 Panobinostat (20 mg/kg) 腹腔注射给携带人 SCLC 肿瘤 H526、BKT、RG1 或 H69 的 SCID 小鼠,每周五次,持续两周。
结果:Panobinostat 显著减缓源于 SCLC 细胞的肿瘤的体内生长并诱导缓解。[1]
方法:为研究对中风后增强运动功能恢复的潜力,将 Panobinostat (3-10 mg/kg) 腹腔注射给中风的 CD-1 小鼠,每两天一次,持续十天。
结果:体育锻炼与 Panobinostat 的结合都不会对中风后小鼠的运动恢复产生实质性影响。Panobinostat 治疗加上有限的身体康复不太可能为患有运动功能障碍的中风幸存者提供治疗方式。[3]
细胞实验 Blasts from peripheral blood of 2 patients and from bone marrow of 4 patients were isolated with Ficoll-Hypaque, put in culture at a density of 500?000 cells/mL with RPMI-1640 medium containing 10% fetal bovine serum and 50 units/mL penicillin and streptomycin, and treated with different doses of LBH589 (0-100 μM) for up to 48 hours [1].
动物实验 AE17 and TC-1 cancer cells (1 × 10^6 cells) were injected into the flanks of adult female C57Bl/6 mice and severe combined immunodeficiency (SCID) mice. M30 (10 × 10^6 cells), A549 (5 × 10^6 cells), H69 (2.5 × 10^6 cells), BK-T (6.5 × 10^6), H526 (10 × 10^6), and RG1 (10 × 10^6) cells were also injected, but in the presence of matrigel (BD Biosciences), into the flanks of SCID mice. There were 5 to 10 mice in each treatment group. The experiments with the A549 and H69 cell lines were repeated to ensure the statistical consistency of the results. Experiments were terminated when the tumors in the control mice had grown to a size that threatened the quality of life of the mice. When tumors reached 100 to 500 mm3, panobinostat was administered via i.p. injections (10–20 mg/kg) on a daily schedule (5-days-on, 2-days-off regimen) for the entire duration of the experiment. Control mice received i.p. injections with dextrose 5% in water ("vehicle treatment"). Every tumor was measured with a caliper at least twice weekly. For evaluation of the effects of combination therapy on SCLC-derived tumors, SCID mice with H69 tumors were administered panobinostat as described above. Three days after the initiation of panobinostat, and again 1 wk later, etoposide (40 mg/kg) was administered i.p [3].
别名 帕比司他, NVP-LBH589, LBH589
分子量 349.43
分子式 C21H23N3O2
CAS No. 404950-80-7

存储

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

溶解度

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

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

DMSO: 64 mg/mL (183.2 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 2.8618 mL 14.309 mL 28.618 mL 71.5451 mL
5 mM 0.5724 mL 2.8618 mL 5.7236 mL 14.309 mL
10 mM 0.2862 mL 1.4309 mL 2.8618 mL 7.1545 mL
20 mM 0.1431 mL 0.7155 mL 1.4309 mL 3.5773 mL
50 mM 0.0572 mL 0.2862 mL 0.5724 mL 1.4309 mL
100 mM 0.0286 mL 0.1431 mL 0.2862 mL 0.7155 mL

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TargetMol Library Books参考文献

1. Crisanti MC, et al. The HDAC inhibitor panobinostat (LBH589) inhibits mesothelioma and lung cancer cells in vitro and in vivo with particular efficacy for small cell lung cancer. Mol Cancer Ther. 2009 Aug;8(8):2221-31. 2. Scuto A, et al. The novel histone deacetylase inhibitor, LBH589, induces expression of DNA damage response genes and apoptosis in Ph- acute lymphoblastic leukemia cells. Blood. 2008 May 15;111(10):5093-100. 3. Al Shoyaib A, et al. The Effect of Histone Deacetylase Inhibitors Panobinostat or Entinostat on Motor Recovery in Mice After Ischemic Stroke. Neuromolecular Med. 2021 Dec;23(4):471-484. 4. Ocio EM, et al. In vitro and in vivo rationale for the triple combination of panobinostat (LBH589) and dexamethasone with either bortezomib or lenalidomide in multiple myeloma. Haematologica. 2010 May;95(5):794-803. 5. Wellinger L C, Hogg S J, Newman D M, et al. BET Inhibition Enhances TNF Mediated Anti-Tumor Immunity[J]. bioRxiv. 2021 6. Juarez-Mercado K E, Prieto-Martinez F D, Sanchez-Cruz N, et al. DNA Methyltransferase Inhibitors with Novel Chemical Scaffolds[J]. bioRxiv. 2020 7. Juárez-Mercado K E, Prieto-Martínez F D, Sánchez-Cruz N, et al. Expanding the Structural Diversity of DNA Methyltransferase Inhibitors[J]. Pharmaceuticals. 2021, 14(1): 17.

TargetMol Library Books文献引用

1. Wellinger L C, Hogg S J, Newman D M, et al. BET Inhibition Enhances TNF Mediated Anti-Tumor Immunity. Cancer Immunology Research. 2022, 10(1): 87-107. 2. Wellinger L C, Hogg S J, Newman D M, et al. Bet inhibition enhances TNF-mediated antitumor immunity. Cancer Immunology Research. 2022, 10(1): 87-107 3. Juárez-Mercado K E, Prieto-Martínez F D, Sánchez-Cruz N, et al. Expanding the Structural Diversity of DNA Methyltransferase Inhibitors. Pharmaceuticals. 2021, 14(1): 17. 4. Zhao F, Huang Y, Zhang Y, et al. SQLE inhibition suppresses the development of pancreatic ductal adenocarcinoma and enhances its sensitivity to chemotherapeutic agents in vitro. Molecular Biology Reports. 2022: 1-9 5. Han L, Song B, Zhang P, et al.PC3T: a signature-driven predictor of chemical compounds for cellular transition.Communications Biology.2023, 6(1): 989.
Epirubicin hydrochloride AOH1160 Sinomenine hydrochloride Xanthoangelol Poziotinib Fosbretabulin Disodium Nimbolide AKT inhibitor VIII

相关化合物库

该产品包含在如下化合物库中:
抗癌药物库 抗癌上市药物库 抗癌临床化合物库 EMA 上市药物库 抗癌活性化合物库 抑制剂库 药物功能重定位化合物库 FDA上市及药典收录分子库 共价抑制剂库 组蛋白修饰化合物库

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Keywords

Panobinostat 404950-80-7 Apoptosis Autophagy Chromatin/Epigenetic DNA Damage/DNA Repair Microbiology/Virology Proteases/Proteasome HIV Protease HDAC Human immunodeficiency virus Histone deacetylases 帕比司他 NVP-LBH 589 HIV inhibit Inhibitor NVP-LBH589 LBH-589 LBH589 NVP-LBH-589 LBH 589 inhibitor

 

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