Panobinostat (LBH589)

製品コードS1030 バッチS103013

印刷

化学情報

Chemical Structure Synonyms NVP-LBH589 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C21H23N3O2
分子量 349.43 CAS No. 404950-80-7
Solubility (25°C)* 体外 DMSO 70 mg/mL (200.32 mM)
Water Insoluble
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Panobinostat (LBH589, NVP-LBH589) is a novel broad-spectrum HDAC inhibitor with IC50 of 5 nM in a cell-free assay. Panobinostat (LBH589) induces autophagy and apoptosis. Panobinostat effectively disrupts HIV latency in vivo. Phase 3.
in vitro Panobinostat (LBH589) induces apoptosis among MOLT-4 and Reh cells in a time- and dose-dependent manner, and is more potent in MOLT-4 than in Reh cells. It markedly prevents the growth of both cell lines in a dose-dependent manner at 48 hours, and causes a 2- to 3-fold increase in the number of cells in the G2/M phase of the cell cycle compared with the control cells. This compound is associated with induction of histone H3K9 and histone H4K8 acetylation as well as decreasing levels of c-Myc expression in a dose-dependent manner. Its treatment also increases the levels of p21 expression, and decreases the levels of c-Myc after an initial increase at the lowest dose (10 nM) in Reh cells. In addition, it gives rise to substantial increases in mRNA levels of proapoptosis and DNA repair genes, and induces increased levels of acetylated histone H3 and H4 at the GADD45G promoter. [1] Besides, it inhibits growth of non small cell lung cancer cell lines (such as human H1299, L55 and A549 with IC50 of 5 nM, 11 nM and 30 nM, respectively), mesothelioma (such as human OK-6 and Ok-5 with IC50 of 5 nM and 7 nM, respectively) and small cell lung cancer cell lines (such as human RG-1 and LD-T with IC50 of 4 nM and 5 nM, respectively). [2]
in vivo Panobinostat (LBH589) markedly decreases tumor growth by 62% in lung cancer and mesothelioma animal models. It is equally effective in immunocompetent and severe combined immunodeficient mice, suggesting that the inhibition of tumor growth by this compound is not due to direct immunologic effects. Daily administration given i.p. at 20 mg/kg for 5 days per week leads to an average decrease in growth of 70%. Compared with the corresponding control tumors, it leads to a 53% decrease for H526-derived tumors, an 81% decrease for BK-T-derived tumors, a 76% decrease for RG-1-derived tumors, and a 70% decrease for H69-derived tumors. In contrast to the lack of tumor regression noted in NSCLC and Meso-derived xenografted tumors that are treated under identical conditions and doses, this compound results in dramatic tumor regression in SCLC-derived tumors and RG-1-derived tumor. [2]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 MOLT-4 cell lines and Reh (pre-B cells)
濃度 50 nM
反応時間 48 hours
実験の流れ Panobinostat (LBH589)-treated and untreated cells [human Ph- acute lymphoblastic leukemia MOLT-4 (T cells) and Reh (pre-B cells)] are stained with annexin V and propidium iodide using annexin V-FITC apoptosis detection kit I. The percentage of apoptotic and nonviable cells is determined by flow cytometry. At least 5 × 104 cells are collected with a CyAn ADP Violet cytometer. Percentage apoptosis is calculated considering all the annexin V-positive plus the annexin V/PI-positive cells; percentage loss of cell viability is calculated considering all the annexin V-positive plus the PI-positive and the annexinV/PI-positive cells.
動物実験 動物モデル Severe combined immunodeficiency (SCID) mice with M30 (107 cells) or A549 (5 × 106 cells), H69 (2.5 × 106 cells), BK-T (6.5 × 106), H526 (10 × 106), and RG1 (10 × 106) cells
投薬量 10 mg/kg, 20 mg/kg
投与方法 Administered via i.p. injection

参考

  • https://pubmed.ncbi.nlm.nih.gov/18349321/
  • https://pubmed.ncbi.nlm.nih.gov/19671764/
  • https://pubmed.ncbi.nlm.nih.gov/19951978/
  • https://pubmed.ncbi.nlm.nih.gov/16740717/
  • https://pubmed.ncbi.nlm.nih.gov/19344997/

カスタマーフィードバック

Data from [Breast Cancer Res Treat , 2012, 131, 777-789]

Data from [PLoS One, 2011, 6, e17138]

Data from [PLoS One, 2011, 6, e17138]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Proteogenomic characterization of non-functional pancreatic neuroendocrine tumors unravels clinically relevant subgroups [ Cancer Cell, 2025, 43(4):776-796.e14] PubMed: 40185092
Molecular mechanisms of unique therapeutic potential of CUDC-907 for MEF2D fusion-driven BCP-ALL [ Signal Transduct Target Ther, 2025, 10(1):230] PubMed: 40695793
Blood and tissue HIV-1 reservoirs display plasticity and lack of compartmentalization in virally suppressed people [ Nat Commun, 2025, 16(1):2173] PubMed: 40038305
Intratumor heterogeneity of EGFR expression mediates targeted therapy resistance and formation of drug tolerant microenvironment [ Nat Commun, 2025, 16(1):28] PubMed: 39747003
Gut microbial metabolite 4-hydroxybenzeneacetic acid drives colorectal cancer progression via accumulation of immunosuppressive PMN-MDSCs [ J Clin Invest, 2025, 135(11)e181243] PubMed: 40179015
Spatial covariance reveals isothiocyanate natural products adjust redox stress to restore function in alpha-1-antitrypsin deficiency [ Cell Rep Med, 2025, 6(1):101917] PubMed: 39809267
A patient-derived T cell lymphoma biorepository uncovers pathogenetic mechanisms and host-related therapeutic vulnerabilities [ Cell Rep Med, 2025, S2666-3791(25)00102-8] PubMed: 40147445
B cell receptor silencing reveals origin and dependencies of high-grade B cell lymphomas with MYC and BCL2 rearrangements [ Blood Cancer Discov, 2025, 10.1158/2643-3230.BCD-25-0099] PubMed: 40402557
Dual targeting of CDK6 and LSD1 is synergistic and overcomes differentiation blockade in AML [ EMBO Mol Med, 2025, 10.1038/s44321-025-00296-2] PubMed: 40883610
HDAC and MEK inhibition synergistically suppresses HOXC6 and enhances PD-1 blockade efficacy in BRAFV600E-mutant microsatellite stable colorectal cancer [ J Immunother Cancer, 2025, 13(1)e010460] PubMed: 39800382

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。