Panobinostat

产品编号: T2383 别名:

帕比司他,NVP-LBH589,LBH589

Panobinostat 是口服非选择性HDAC抑制剂，具有抗肿瘤活性。它诱导细胞凋亡和自噬，可研究难治性或复发性多发性骨髓瘤。

陶术生物的所有产品和服务仅用于科学研究，我们不为任何个人用途提供产品和服务。

CAS：404950-80-7

规格	库存	价格/RMB	数量
{{item.packagingtext}}	{{item.goodshuoqi}}	{{item.moneyunit}} {{item.finalprice}} {{item.pricetext==null\|\|item.pricetext==''?pricetext:item.pricetext}}

生物活性化学信息储存和溶解度信息参考文献引用文献

产品描述

Panobinostat is a potent inhibitor of all HDACs (Kis: 0.6-31 nM for HDAC1-11).

体外活性

Low nanomolar concentrations (IC50: 5-20 nM) of Panobinostat (LBH589) induced cell-cycle arrest, apoptosis, and histone (H3K9 and H4K8) hyperacetylation. LBH589 treatment increased mRNA levels of proapoptosis, growth arrest, and DNA damage repair genes including FANCG, FOXO3A, GADD45A, GADD45B, and GADD45G [1]. LBH589 induces acetylation of histone H3 and H4 and of hsp90, increases p21 levels, as well as induces cell-cycle G(1) phase accumulation and apoptosis of the human chronic myeloid leukemia blast crisis (CML-BC) K562 cells and acute leukemia MV4-11 cells with the activating length mutation of FLT-3 [2]. Panobinostat was cytotoxic in almost all 37 cancer cell lines tested. IC50 and LD50 values were in the low nmol/L range (4-470 nmol/L; median, 20 nmol/L). Small cell lung cancer (SCLC) cell lines were among the most sensitive lines, with LD(50) values consistently <25 nmol/L [3].

体内活性

In lung cancer and mesothelioma animal models, panobinostat significantly decreased tumor growth by an average of 62% when compared with vehicle control. Panobinostat was equally effective in immunocompetent and severe combined immunodeficiency mice. Panobinostat was, however, particularly effective in SCLC xenografts, and the addition of the chemotherapy agent etoposide augmented antitumor effects [3]. In all three dosed groups (5, 10 and 20 mg/kg i.p.), panobinostat demonstrated a clear benefit of decreased tumor burden, statistically significant differences were seen for groups treated with 10 and 20 mg/kg doses, as compared with the vehicle control group. Panobinostat treatment also significantly improved TTE, especially at the 20 mg/kg dose [4].

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].

Cas No.

404950-80-7

分子式

C21H23N3O2

分子量

349.434

别名

帕比司他;NVP-LBH589;LBH589;Panobinostat

参考文献

[1]Juarez-Mercado K E, Prieto-Martinez F D, Sanchez-Cruz N, et al. DNA Methyltransferase Inhibitors with Novel Chemical Scaffolds[J]. bioRxiv. 2020 [2]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.[3]Wellinger L C, Hogg S J, Newman D M, et al. BET Inhibition Enhances TNF Mediated Anti-Tumor Immunity[J]. bioRxiv. 2021 [4]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.[5]George P, et al. Combination of the histone deacetylase inhibitor LBH589 and the hsp90 inhibitor 17-AAG is highly active against human CML-BC cells and AML cells with activating mutation of FLT-3. Blood. 2005 Feb 15;105(4):1768-76.[6]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.[7]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.

引用文献

[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

储存和溶解度

H2O:<1 mg/mL
Ethanol:<1 mg/mL
DMSO:64 mg/mL (183.2 mM)

Powder: -20°C for 3 years
In solvent: -80°C for 2 years

剂量换算 Panobinostat 404950-80-7

对于各种应用，安全且有效的用药剂量是很有必要的了解更多

体内实验配液计算器

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 ul

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 +

% +

% Tween 80 +

% ddH₂O

% DMSO +

重置计算

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 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 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

计算器

摩尔计算器可以帮助您计算

制备已知体积和浓度溶液所需的化合物质量
将已知质量的化合物溶解到所需浓度所需的溶液体积
已知质量的化合物在一定体积内形成的溶液的浓度

质量

浓度

体积

分子量

重置计算

稀释计算器可以帮助您计算

制备已知体积和浓度溶液所需的化合物质量
将已知质量的化合物溶解到所需浓度所需的溶液体积
已知质量的化合物在一定体积内形成的溶液的浓度

浓度（起始）

体积（起始）

浓度（终点）

体积（终点）

重置计算

配液计算器可以帮助您计算

重组计算器可帮助您快速计算试剂的体积，以重组您的小瓶。

溶液体积

质量

配液浓度

重置计算

配液计算器可以帮助您计算

输入化合物的化学式以计算其摩尔质量和元素组成
提示：化学式需区分大小写

分子结构式

总分子量

g/mol

重置计算

技术支持

在抑制剂处理说明中可以找到您可能遇到的问题的答案。主题包括如何准备储备溶液，如何存储产品以及基于细胞的测定和动物实验需要特别注意的问题。

Keywords

LBH 589 Human immunodeficiency virus Histone deacetylases 帕比司他 HIV HDAC LBH-589 Autophagy inhibit Panobinostat NVP-LBH589 Inhibitor Apoptosis LBH589 404950-80-7

Panobinostat 相关推荐

相关化合物库推荐该产品包含在如下化合物库中：

注册成功

Panobinostat

帕比司他,NVP-LBH589,LBH589

摩尔计算器可以帮助您计算

稀释计算器可以帮助您计算

配液计算器可以帮助您计算

配液计算器可以帮助您计算