ホームページ Epigenetics HDAC inhibitor - Autophagy activator Belinostat For research use only.

Belinostat

別名：PXD101,NSC726630, PX-105684

Belinostat is a novel HDAC inhibitor with IC50 of 27 nM in a cell-free assay, with activity demonstrated in cisplatin-resistant tumors. Belinostat (PXD101) induces autophagy.

Belinostat化学構造

CAS No. 866323-14-0

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 29500 国内在庫あり
JPY 22000 国内在庫あり
JPY 55500 国内在庫あり
JPY 145500 国内在庫あり
JPY 220500 国内在庫なし(納期7~10日)

代表番号: 045-509-1970|電子メール：[email protected]
よく尋ねられる質問

文献中Selleckの製品使用例（95）

製品安全説明書

現在のバッチを見る： 純度： 99.74%
99.74

Belinostat関連製品

シグナル伝達経路

HDAC Signaling Pathways

HDACシグナル伝達経路

HDAC阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
PC9 Function Assay 500 nM 24 h decreases EGFR expression 23515752
H460 Function Assay 0.5/1/2 μM 4 h inhibits the levels of Akt (p-Akt) and EGFR 23515752
H1650 Function Assay 0.5/1/2 μM 4 h inhibits the levels of Akt (p-Akt) and EGFR 23515752
PC9 Function Assay 0.5/1/2 μM 4 h inhibits the levels of Akt (p-Akt) and EGFR 23515752
Panc0327 Apoptosis Assay 1 μM 24 h induces apoptosis 23475695
Panc1005 Apoptosis Assay 1 μM 24 h induces apoptosis 23475695
Panc0403 Apoptosis Assay 1 μM 24 h induces apoptosis 23475695
AsPc1 Function Assay 1/10 μM 24 h induces growth arrested in G2/M 23475695
MiaPaCa2 Function Assay 1/10 μM 24 h induces growth arrested in G2/M 23475695
T3M4 Growth Inhibition Assay 0-800 nM 48 h inhibits cell proliferation in a dose dependent manner 22681698
AsPC-1 Growth Inhibition Assay 0-800 nM 48 h inhibits cell proliferation in a dose dependent manner 22681698
Panc-1  Growth Inhibition Assay 0-800 nM 48 h inhibits cell proliferation in a dose dependent manner 22681698
T3M4 Apoptosis Assay 100/500/1000 nM 48 h induces dose dependent apoptosis 22681698
AsPC-1 Apoptosis Assay 100/500/1000 nM 48 h induces dose dependent apoptosis 22681698
Panc-1  Apoptosis Assay 100/500/1000 nM 48 h induces dose dependent apoptosis 22681698
HCT116 Function Assay 0.9 μM  24 h down-regulats TS protein levels after 6 h incubation 17124594
H1650 Function Assay 500 nM 24 h decreases EGFR expression 23515752
H460 Function Assay 500 nM 24 h decreases EGFR expression 23515752
PANC-1 Function Assay 10 μM 2/4 h increases intracellular ROS level 23743198
PANC-1 Cell Viability Assay 1/10 μM 48 h decreases cell viability in a dose dependent manner 23743198
PANC-1 Function Assay 10 μM 2/4/6 h induces AMPK activation 23743198
HL-60  Function Assay 0.2 μM 24/48/72 h enhances RA-induced granulocytic differentiation 25864732
NB4 Function Assay 0.2 μM 24/48/72 h enhances RA-induced granulocytic differentiation 25864732
HL-60  Function Assay 2 μM 24/48 h blocks cell cycle in S phase 25864732
NB4 Function Assay 2 μM 24/48 h blocks cell cycle in S phase 25864732
HL-60  Cell Viability Assay 0.2/2 μM 24/48/72 h decreases cell viability in both time and dose dependent manner 25864732
NB4 Cell Viability Assay 0.2/2 μM 24/48/72 h decreases cell viability in both time and dose dependent manner 25864732
Huh-luc/neo7 Function assay 1 uM 1 to 3 hrs Inhibition of HDAC class 1 in human Huh-luc/neo7 cells assessed as histone H3 acetylation at 1 uM after 1 to 3 hrs by Western blotting analysis 25937017
PC3 Function assay 0.3 uM 48 hrs Inhibition of HDAC in human PC3 cells assessed as increase in amount of acetylated histone H3 at 0.3 uM after 48 hrs by Western blot analysis 27344487
HCT116 Function assay 0.3 uM 48 hrs Inhibition of HDAC in human HCT116 cells assessed as increase in amount of acetylated histone H3 at 0.3 uM after 48 hrs by Western blot analysis 27344487
AsPc1 Growth Inhibition Assay 48 h EC50=0.3 μM 23475695
Panc0327 Growth Inhibition Assay 48 h EC50=0.5 μM 23475695
MiaPaCa2 Growth Inhibition Assay 48 h EC50=0.7 μM 23475695
BxPc3 Growth Inhibition Assay 48 h EC50=1.0 μM 23475695
Panc0403 Growth Inhibition Assay 48 h EC50=1.1 μM 23475695
Panc1005 Growth Inhibition Assay 48 h EC50=1.1 μM 23475695
PL45 Growth Inhibition Assay 48 h EC50=20.8 μM 23475695
Panc0203 Growth Inhibition Assay 48 h EC50=22.2 μM 23475695
HBL-2 Growth Inhibition Assay 24 h IC50=0.4 μM 20068080
Jeko-1 Growth Inhibition Assay 24 h IC50=0.2 μM 20068080
Granta-519 Growth Inhibition Assay 24 h IC50=56.3 μM 20068080
HCT116 Growth Inhibition Assay 48 h EC50=0.28 μM 17124594
HCC4006 Growth Inhibition Assay 72 h IC50=0.46 μM 23515752
HCC2935 Growth Inhibition Assay 72 h IC50=0.97 μM 23515752
HCC827 Growth Inhibition Assay 72 h IC50=0.29 μM 23515752
HCC2279 Growth Inhibition Assay 72 h IC50=0.4 μM 23515752
PC9 Growth Inhibition Assay 72 h IC50=0.29 μM 23515752
H820 Growth Inhibition Assay 72 h IC50=0.4 μM 23515752
H1650 Growth Inhibition Assay 72 h IC50=0.88 μM 23515752
H1975 Growth Inhibition Assay 72 h IC50=0.68 μM 23515752
H520 Growth Inhibition Assay 72 h IC50=0.75 μM 23515752
H1299 Growth Inhibition Assay 72 h IC50=1.2 μM 23515752
H460 Growth Inhibition Assay 72 h IC50=0.86 μM 23515752
H1666 Growth Inhibition Assay 72 h IC50>10 μM 23515752
RAW264.7 Anti-inflammatory assay 1 hr Anti-inflammatory activity in LPS-stimulated mouse RAW264.7 cells assessed as suppression of IL6 production pre-incubated for 1 hr before LPS stimulation for 24 hrs by ELISA method, IC50 = 0.000059 μM. 25113875
HeLa Function assay 30 mins Inhibition of HDAC in human HeLa cells nuclear extracts incubated for 30 mins by fluorescent assay, IC50 = 0.0264 μM. 25113875
MDA-MB-231 Antiproliferative assay 72 hrs Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by resazurin dye based fluorescence assay, IC50 = 0.062 μM. 29456804
Jurkat Antiproliferative assay 48 hrs Antiproliferative activity against human Jurkat cells after 48 hrs by MTT assay, IC50 = 0.07 μM. 29533873
A549 Antiproliferative assay 72 hrs Antiproliferative activity against human A549 cells after 72 hrs by resazurin dye based fluorescence assay, IC50 = 0.077 μM. 29456804
HeLa Antiproliferative assay 72 hrs Antiproliferative activity against human HeLa cells after 72 hrs by resazurin dye based fluorescence assay, IC50 = 0.087 μM. 29456804
MCF7 Antiproliferative assay 72 hrs Antiproliferative activity against human MCF7 cells after 72 hrs by resazurin dye based fluorescence assay, IC50 = 0.096 μM. 29456804
HEL Antiproliferative assay 48 hrs Antiproliferative activity against human HEL cells after 48 hrs by MTT assay, IC50 = 0.1 μM. 29533873
Huh7 Antiviral assay 3 days Antiviral activity against HCV genotype 1b infected in human Huh7 cells after 3 days by luciferase reporter gene assay, EC50 = 0.12 μM. 25490700
HCT116 Antiproliferative assay 48 hrs Antiproliferative activity against human HCT116 cells after 48 hrs by SRB assay, GI50 = 0.13 μM. 27344487
MOLT4 Antiproliferative assay 48 hrs Antiproliferative activity against human MOLT4 cells after 48 hrs by MTT assay, IC50 = 0.14 μM. 29533873
SK-N-BE(2) Antiproliferative assay 48 hrs Antiproliferative activity against human SK-N-BE(2) cells after 48 hrs by MTT assay, IC50 = 0.31 μM. 29533873
PC3 Antiproliferative assay 48 hrs Antiproliferative activity against human PC3 cells after 48 hrs by SRB assay, GI50 = 0.39 μM. 27344487
PC3 Antiproliferative assay 96 hrs Antiproliferative activity against human PC3 cells after 96 hrs by celltiter 96 assay, IC50 = 0.45 μM. 21634430
HeLa Antiproliferative assay 48 hrs Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay, IC50 = 0.51 μM. 29533873
HCT116 Antiproliferative assay 96 hrs Antiproliferative activity against human HCT116 cells after 96 hrs by celltiter 96 assay, IC50 = 0.6 μM. 21634430
A2780 Antiproliferative assay 96 hrs Antiproliferative activity against human A2780 cells after 96 hrs by celltiter 96 assay, IC50 = 0.67 μM. 21634430
HuH7 Cytotoxicity assay 3 days Cytotoxicity against human HuH7 cells assessed as inhibition of cell viability after 3 days by CellTiter 96 assay, CC50 = 0.68 μM. 25490700
COLO205 Antiproliferative assay 96 hrs Antiproliferative activity against human COLO205 cells after 96 hrs by celltiter 96 assay, IC50 = 0.7 μM. 21634430
A549 Antiproliferative assay 48 hrs Antiproliferative activity against human A549 cells after 48 hrs by SRB assay, GI50 = 0.78 μM. 27344487
HL60 Antiproliferative assay 48 hrs Antiproliferative activity against human HL60 cells after 48 hrs by SRB assay, GI50 = 1.09 μM. 27344487
K562 Antiproliferative assay 48 hrs Antiproliferative activity against human K562 cells after 48 hrs by MTT assay, IC50 = 1.1 μM. 29533873
PC3 Antiproliferative assay 48 hrs Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay, IC50 = 1.3 μM. 29533873
NFF Cytotoxicity assay 72 hrs Cytotoxicity against human NFF cells after 72 hrs by SRB assay, IC50 = 1.4 μM. 28241112
HEK293 Cytotoxicity assay 48 hrs Cytotoxicity against HEK293 cells after 48 hrs by resazurin assay, IC50 = 1.4 μM. 28241112
NFF Cytotoxicity assay 72 hrs Cytotoxicity against human NFF cells after 72 hrs by sulforhodamine B assay, IC50 = 1.42 μM. 30245402
HEK293 Cytotoxicity assay 48 hrs Cytotoxicity against HEK293 cells after 48 hrs by resazurin dye based assay, IC50 = 1.42 μM. 30245402
RAW264.7 Anti-inflammatory assay 1 hr Anti-inflammatory activity in LPS-stimulated mouse RAW264.7 cells assessed as suppression of nitric oxide production pre-incubated for 1 hr before LPS stimulation for 24 hrs by Griess reagent based assay, IC50 = 2.2 μM. 25113875
RAW264.7 Anti-inflammatory assay 1 hr Anti-inflammatory activity in LPS-stimulated mouse RAW264.7 cells assessed as suppression of TNFalpha production pre-incubated for 1 hr before LPS stimulation for 24 hrs by ELISA method, IC50 = 4.7 μM. 25113875
RAW264.7 Anti-inflammatory assay 1 hr Anti-inflammatory activity in LPS-stimulated mouse RAW264.7 cells assessed as suppression of PGE2 production pre-incubated for 1 hr before LPS stimulation for 24 hrs by enzyme immunoassay method, IC50 = 8.28 μM. 25113875
HEK293 Function assay Inhibition of HDAC6 in HEK293 cells, IC50 = 0.015 μM. 18308563
HEK293 Function assay Inhibition of HDAC1 in HEK293 cells, IC50 = 0.018 μM. 18308563
HeLa Function assay Inhibition of HDAC in human HeLa cells using Fluor de Lys as substrate by fluorescence assay, IC50 = 0.027 μM. 23639537
HeLa Function assay Inhibition of HDAC from human HeLa cells, IC50 = 0.028 μM. 18247554
HEK293 Function assay Inhibition of HDAC3 in HEK293 cells, IC50 = 0.046 μM. 18308563
HCT116 Antiproliferative assay Antiproliferative activity against human HCT116 cells assessed as growth inhibition, IC50 = 0.16 μM. 21650221
HCT116 Antiproliferative assay Antiproliferative activity against human HCT116 cells, IC50 = 0.16 μM. 21742496
H1299 Antiproliferative assay Antiproliferative activity against human H1299 cells, IC50 = 0.46 μM. 21650221
他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

生物活性

製品説明 Belinostat is a novel HDAC inhibitor with IC50 of 27 nM in a cell-free assay, with activity demonstrated in cisplatin-resistant tumors. Belinostat (PXD101) induces autophagy.
特性 Lead compound of Topotarget.
Targets
HDAC [1]
(Cell-free assay)
27 nM
In Vitro
In vitro Belinostat inhibits the growth of tumor cells (A2780, HCT116, HT29, WIL, CALU-3, MCF7, PC3 and HS852) with IC50 from 0.2-0.66 μM. PD101 shows low activity in A2780/cp70 and 2780AD cells, which are cisplatin and doxorubicin-resistant derivatives of A2780 cells. Belinostat could induce apoptosis through PARP cleavage and acetylation of histones H3/H4. [1] Belinostat inhibits bladder cancer cell growth, especially in 5637 cells, which shows accumulation of G0-G1 phase, decrease in S phase and increase in G2-M phase. [2] The growth inhibitory activity of belinostat on cell lines is not strongly influenced by the multidrug-resistant phenotype, whereas the activity of docetaxel is clearly affected. Belinostat could enhance the growth inhibitory activity of docetaxel or carboplatin in OVCAR-3 and A2780 cells. Belinostat also shows enhanced tubulin acetylation in ovarian cancer cell lines. [3] A recent study shows that Belinostat activates protein kinase A in a TGF-β signaling-dependent mechanism and decreases survivin mRNA. [4]
Kinase Assay 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 H2O is gently applied, and three drop fractions are collected; this is repeated until 4–5 mL of distilled H2O 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.
細胞実験 細胞株 A2780, A2780/cp70, 2780AD, HCT116, HT29, WIL, CALU-3, MCF7, PC3 and HS852
濃度 0.016 - 10 μM
反応時間 24 hours
実験の流れ 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.
実験結果図 Methods Biomarkers 結果図 PMID
Western blot p-H2AX(Ser139) / KU70 / KU80 / RAD51 / RAD52 / ERCC1 Acetyl Histone H3 / Acetyl Histone H4 / Acetyl tubulin p21 / p27 SOS1 / SOS2 PARP / p-ERK / p-p38 / p38 / p-BRAF / p-MEK / MEK 24155971
Growth inhibition assay Cell viability IC50 24155971
In Vivo
In Vivo Belinostat indicates significant tumor growth delay in A2780 and A2780/cp70 xenograft at a dose of 10mg/kg with no effects on the body weight. [1] Belinostat also induces p21WAF1, HDAC core and cell communication genes in mouse bladder tumors. [2] Belinostat monotherapy induces dose-proportional antitumor effects with TGI of 47% at a dose of 100mg/kg in A2780 xenograft. The combination of Belinostat (100 mg/kg) with carboplatin (40 mg/kg) could delay tumor growth from 18.6 days to 22.5 days. [3] Combining with bortezomib, Belinostat results in great tumor inhibition and gastrointestinal toxicity in mice with bortezomib-resistant UMSCC-11A xenograft. [5]
動物実験 動物モデル A2780, A2780/cp70 and HCT116 cells are injected s.c. into the right flank of CD1 nu/nu mice.
投与量 ≤40 mg/kg
投与経路 Administered via i.p.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06406465 Not yet recruiting
Carcinoma Neuroendocrine|Tumor Neuroendocrine|Tumors Neuroendocrine|Neuroendocrine; Carcinoma|Small Cell; Receptors
National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC)
 May 15 2024 Phase 2
NCT04315233 Recruiting
Metastatic Breast Cancer|Recurrent Ovarian Carcinoma
University of Utah|Novartis|Acrotech Biopharma
 May 3 2021 Phase 1
NCT04703920 Recruiting
Metastatic Breast Cancer|Metastatic Castration-resistant Prostate Cancer|Metastatic Ovarian Carcinoma
University of Michigan Rogel Cancer Center|Pfizer|Acrotech Biopharma Inc.
 March 4 2021 Phase 1
NCT03772925 Active not recruiting
Recurrent Acute Myeloid Leukemia|Recurrent Myelodysplastic Syndrome|Refractory Acute Myeloid Leukemia|Refractory Myelodysplastic Syndrome
National Cancer Institute (NCI)
 June 20 2019 Phase 1

化学情報

分子量 318.35 化学式

C15H14N2O4S
CAS No. 866323-14-0 SDF Download Belinostat SDFをダウンロードする
Smiles C1=CC=C(C=C1)NS(=O)(=O)C2=CC=CC(=C2)C=CC(=O)NO
保管

In vitro
Batch:

DMSO : 64 mg/mL ( (201.03 mM)； 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

mg/kg g μL 匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH2O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

* 必須

大学・企業名を記入してください
名前を記入してください
電子メール・アドレスを記入してください 有効なメールアドレスを入力してください
お問い合わせ内容をご入力ください

よくある質問（FAQ）

質問1:
Could you please give some suggestions for the use of Belinostat in vivo (i.p. injection)?

回答
For I.P. injection, S1085 Belinostat (PXD101) can be dissolved in 2% DMSO+30% PEG 300+ddH2O at 10 mg/ml clearly. When preparing the solution, please dissolve the compound in DMSO clearly first. Then add PEG, after they mixed well, then dilute with water. Hope this information is useful to you.

Tags: Belinostatを買う | Belinostat ic50 | Belinostat供給者 | Belinostatを購入する | Belinostat費用 | Belinostat生産者 | オーダーBelinostat | Belinostat化学構造 | Belinostat分子量 | Belinostat代理店