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Belinostat [866323-14-0]

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Referencia HY-10225-10mg

embalaje : 10mg

Contact local distributor :

Teléfono : +1 850 650 7790

Marca : MedChemExpress

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Contact local distributor :

Teléfono : +1 850 650 7790

Descripciòn

Belinostat (PXD101; PX105684) is a potent HDAC inhibitor with an IC₅₀ of 27 nM in HeLa cell extracts.

IC₅₀ & Target^[1]^[2]

HDAC6

82 nM (IC₅₀)

HDAC

27 nM (IC₅₀, Hela cell)

Cellular Effect

Cell Line	Type	Value	Description	References
143B	GI₅₀	3.3 μM Compound: 54; PDX-101	Antiproliferative activity against human 143B cells Antiproliferative activity against human 143B cells	[PMID: 37875056]
A2780	IC₅₀	0.67 μM Compound: PXD101	Antiproliferative activity against human A2780 cells after 96 hrs by celltiter 96 assay Antiproliferative activity against human A2780 cells after 96 hrs by celltiter 96 assay	[PMID: 21634430]
A549	GI₅₀	0.23 μM Compound: 3; PXD101	Growth inhibition of human A549 cells after 48 hrs by sulforhodamine B assay Growth inhibition of human A549 cells after 48 hrs by sulforhodamine B assay	[PMID: 28395150]
A549	GI₅₀	0.78 μM Compound: PXD101	Antiproliferative activity against human A549 cells after 48 hrs by SRB assay Antiproliferative activity against human A549 cells after 48 hrs by SRB assay	[PMID: 27344487]
A549	IC₅₀	0.077 μM Compound: 2	Antiproliferative activity against human A549 cells after 72 hrs by resazurin dye based fluorescence assay Antiproliferative activity against human A549 cells after 72 hrs by resazurin dye based fluorescence assay	[PMID: 29456804]
ASPC1	GI₅₀	0.65 μM Compound: 3; PXD101	Growth inhibition of human AsPC1 cells after 48 hrs by sulforhodamine B assay Growth inhibition of human AsPC1 cells after 48 hrs by sulforhodamine B assay	[PMID: 28395150]
COLO 205	IC₅₀	0.7 μM Compound: PXD101	Antiproliferative activity against human COLO205 cells after 96 hrs by celltiter 96 assay Antiproliferative activity against human COLO205 cells after 96 hrs by celltiter 96 assay	[PMID: 21634430]
HCT-116	GI₅₀	0.13 μM Compound: PXD101	Antiproliferative activity against human HCT116 cells after 48 hrs by SRB assay Antiproliferative activity against human HCT116 cells after 48 hrs by SRB assay	[PMID: 27344487]
HCT-116	IC₅₀	0.16 μM Compound: 2, PXD-101	Antiproliferative activity against human HCT116 cells Antiproliferative activity against human HCT116 cells	[PMID: 21742496]
HCT-116	IC₅₀	0.6 μM Compound: PXD101	Antiproliferative activity against human HCT116 cells after 96 hrs by celltiter 96 assay Antiproliferative activity against human HCT116 cells after 96 hrs by celltiter 96 assay	[PMID: 21634430]
HCT-116	IC₅₀	160 nM Compound: 2, PXD101	Antiproliferative activity against human HCT116 cells assessed as growth inhibition Antiproliferative activity against human HCT116 cells assessed as growth inhibition	[PMID: 21650221]
HEK293	IC₅₀	1.4 μM Compound: 33	Cytotoxicity against HEK293 cells after 48 hrs by resazurin assay Cytotoxicity against HEK293 cells after 48 hrs by resazurin assay	[PMID: 28241112]
HEK293	IC₅₀	1420 nM Compound: Belinostat	Cytotoxicity against HEK293 cells after 48 hrs by resazurin dye based assay Cytotoxicity against HEK293 cells after 48 hrs by resazurin dye based assay	[PMID: 30245402]
HEK293	IC₅₀	15 nM Compound: PXD101	Inhibition of HDAC6 in HEK293 cells Inhibition of HDAC6 in HEK293 cells	[PMID: 18308563]
HEK293	IC₅₀	18 nM Compound: PXD101	Inhibition of HDAC1 in HEK293 cells Inhibition of HDAC1 in HEK293 cells	[PMID: 18308563]
HEK293	IC₅₀	46 nM Compound: PXD101	Inhibition of HDAC3 in HEK293 cells Inhibition of HDAC3 in HEK293 cells	[PMID: 18308563]
HEL	IC₅₀	<0.78125 μM Compound: PXD101	Antiproliferative activity against human HEL cells after 48 hrs by MTT assay Antiproliferative activity against human HEL cells after 48 hrs by MTT assay	[PMID: 30879863]
HEL	IC₅₀	0.1 μM Compound: PXD101	Antiproliferative activity against human HEL cells after 48 hrs by MTT assay Antiproliferative activity against human HEL cells after 48 hrs by MTT assay	[PMID: 29533873]
HeLa	IC₅₀	0.087 μM Compound: 2	Antiproliferative activity against human HeLa cells after 72 hrs by resazurin dye based fluorescence assay Antiproliferative activity against human HeLa cells after 72 hrs by resazurin dye based fluorescence assay	[PMID: 29456804]
HeLa	IC₅₀	0.087 μM Compound: PXD101	Inhibition of HDAC in human HeLa nuclear extract using Boc-Lys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence assay Inhibition of HDAC in human HeLa nuclear extract using Boc-Lys(Ac)-AMC as substrate preincubated for 5 mins followed by substrate addition and measured after 30 mins by fluorescence assay	[PMID: 30879863]
HeLa	IC₅₀	0.51 μM Compound: PXD101	Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay	[PMID: 29533873]
HeLa	IC₅₀	1.07 μM Compound: PXD101	Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay	[PMID: 30879863]
HeLa	IC₅₀	10 nM Compound: 25; PXD-101	Inhibition of HDAC in human HeLa cell extracts Inhibition of HDAC in human HeLa cell extracts	[PMID: 31536895]
HeLa	IC₅₀	189 nM Compound: PXD101	Inhibition Class 1 histone deacetylase in human HeLa nuclear extracts using Fluor-de- Lys-green substrate by fluorescence assay Inhibition Class 1 histone deacetylase in human HeLa nuclear extracts using Fluor-de- Lys-green substrate by fluorescence assay	[PMID: 31400937]
HeLa	IC₅₀	26.4 nM Compound: 8, PXD101	Inhibition of HDAC in human HeLa cells nuclear extracts incubated for 30 mins by fluorescent assay Inhibition of HDAC in human HeLa cells nuclear extracts incubated for 30 mins by fluorescent assay	[PMID: 25113875]
HeLa	IC₅₀	27 nM Compound: PXD101	Inhibition of HDAC in human HeLa cells using Fluor de Lys as substrate by fluorescence assay Inhibition of HDAC in human HeLa cells using Fluor de Lys as substrate by fluorescence assay	[PMID: 23639537]
HeLa	IC₅₀	28 nM Compound: 17a, PXD101	Inhibition of HDAC from human HeLa cells Inhibition of HDAC from human HeLa cells	[PMID: 18247554]
HeLa	IC₅₀	81 nM Compound: 3; PXD101	Inhibition of HDAC in human HeLa cell nuclear extract using Ac-Lys(Ac)-pNA as substrate after 30 mins by fluorescence assay Inhibition of HDAC in human HeLa cell nuclear extract using Ac-Lys(Ac)-pNA as substrate after 30 mins by fluorescence assay	[PMID: 28395150]
HL-60	GI₅₀	1.09 μM Compound: PXD101	Antiproliferative activity against human HL60 cells after 48 hrs by SRB assay Antiproliferative activity against human HL60 cells after 48 hrs by SRB assay	[PMID: 27344487]
HOS	GI₅₀	3.3 μM Compound: 54; PDX-101	Antiproliferative activity against human HOS cells Antiproliferative activity against human HOS cells	[PMID: 37875056]
HT-29	IC₅₀	0.86 μM Compound: PXD101	Antiproliferative activity against human HT-29 cells after 48 hrs by MTT assay Antiproliferative activity against human HT-29 cells after 48 hrs by MTT assay	[PMID: 30879863]
Huh-7	CC₅₀	0.65 μM Compound: Belinostat	Cytotoxicity against human HuH7 cells assessed as reduction in cell viability incubated for 3 days by MTT assay Cytotoxicity against human HuH7 cells assessed as reduction in cell viability incubated for 3 days by MTT assay	[PMID: 31201063]
Huh-7	CC₅₀	0.68 μM Compound: 7, PXD101	Cytotoxicity against human HuH7 cells assessed as inhibition of cell viability after 3 days by CellTiter 96 assay Cytotoxicity against human HuH7 cells assessed as inhibition of cell viability after 3 days by CellTiter 96 assay	[PMID: 25490700]
Huh-7	EC₅₀	0.12 μM Compound: 7, PXD101	Antiviral activity against HCV genotype 1b infected in human Huh7 cells after 3 days by luciferase reporter gene assay Antiviral activity against HCV genotype 1b infected in human Huh7 cells after 3 days by luciferase reporter gene assay	[PMID: 25490700]
Jurkat	GI₅₀	0.11 μM Compound: 2	Growth inhibition of human Jurkat cells Growth inhibition of human Jurkat cells	[PMID: 37429084]
Jurkat	IC₅₀	0.07 μM Compound: PXD101	Antiproliferative activity against human Jurkat cells after 48 hrs by MTT assay Antiproliferative activity against human Jurkat cells after 48 hrs by MTT assay	[PMID: 29533873]
K562	IC₅₀	1.07 μM Compound: PXD101	Antiproliferative activity against human K562 cells after 48 hrs by MTT assay Antiproliferative activity against human K562 cells after 48 hrs by MTT assay	[PMID: 30879863]
K562	IC₅₀	1.1 μM Compound: PXD101	Antiproliferative activity against human K562 cells after 48 hrs by MTT assay Antiproliferative activity against human K562 cells after 48 hrs by MTT assay	[PMID: 29533873]
MCF7	IC₅₀	0.096 μM Compound: 2	Antiproliferative activity against human MCF7 cells after 72 hrs by resazurin dye based fluorescence assay Antiproliferative activity against human MCF7 cells after 72 hrs by resazurin dye based fluorescence assay	[PMID: 29456804]
MDA-MB-231	GI₅₀	0.28 μM Compound: 3; PXD101	Growth inhibition of human MDA-MB-231 cells after 48 hrs by sulforhodamine B assay Growth inhibition of human MDA-MB-231 cells after 48 hrs by sulforhodamine B assay	[PMID: 28395150]
MDA-MB-231	IC₅₀	0.062 μM Compound: 2	Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by resazurin dye based fluorescence assay Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by resazurin dye based fluorescence assay	[PMID: 29456804]
MOLT-4	GI₅₀	0.12 μM Compound: 2	Growth inhibition of human MOLT-4 cells measured after 24 hrs by MTT assay Growth inhibition of human MOLT-4 cells measured after 24 hrs by MTT assay	[PMID: 37429084]
MOLT-4	IC₅₀	0.14 μM Compound: PXD101	Antiproliferative activity against human MOLT4 cells after 48 hrs by MTT assay Antiproliferative activity against human MOLT4 cells after 48 hrs by MTT assay	[PMID: 29533873]
NCI-H1299	IC₅₀	460 nM Compound: 2, PXD101	Antiproliferative activity against human H1299 cells Antiproliferative activity against human H1299 cells	[PMID: 21650221]
NCI-H23	IC₅₀	2.53 μM Compound: 54; PDX-101	Antiproliferative activity against human NCI-H23 cells incubated for 48 hrs by colorimetric method Antiproliferative activity against human NCI-H23 cells incubated for 48 hrs by colorimetric method	[PMID: 37875056]
NFF	IC₅₀	1.4 μM Compound: 33	Cytotoxicity against human NFF cells after 72 hrs by SRB assay Cytotoxicity against human NFF cells after 72 hrs by SRB assay	[PMID: 28241112]
NFF	IC₅₀	1420 nM Compound: Belinostat	Cytotoxicity against human NFF cells after 72 hrs by sulforhodamine B assay Cytotoxicity against human NFF cells after 72 hrs by sulforhodamine B assay	[PMID: 30245402]
NFF	IC₅₀	2.37 μM Compound: Belinostat	Cytotoxicity against human NFF cells incubated for 72 hrs by SRB assay Cytotoxicity against human NFF cells incubated for 72 hrs by SRB assay	[PMID: 39208744]
PC-3	GI₅₀	0.31 μM Compound: 3; PXD101	Growth inhibition of human PC3 cells after 48 hrs by sulforhodamine B assay Growth inhibition of human PC3 cells after 48 hrs by sulforhodamine B assay	[PMID: 28395150]
PC-3	GI₅₀	0.39 μM Compound: PXD101	Antiproliferative activity against human PC3 cells after 48 hrs by SRB assay Antiproliferative activity against human PC3 cells after 48 hrs by SRB assay	[PMID: 27344487]
PC-3	IC₅₀	0.45 μM Compound: PXD101	Antiproliferative activity against human PC3 cells after 96 hrs by celltiter 96 assay Antiproliferative activity against human PC3 cells after 96 hrs by celltiter 96 assay	[PMID: 21634430]
PC-3	IC₅₀	1.3 μM Compound: PXD101	Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay	[PMID: 29533873]
PC-3	IC₅₀	1.32 μM Compound: PXD101	Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay	[PMID: 30879863]
PC-3	IC₅₀	2.53 μM Compound: 54; PDX-101	Antiproliferative activity against human PC-3 cells incubated for 48 hrs by colorimetric method Antiproliferative activity against human PC-3 cells incubated for 48 hrs by colorimetric method	[PMID: 37875056]
RAW264.7	IC₅₀	0.059 nM Compound: 8, PXD101	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 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	[PMID: 25113875]
RAW264.7	IC₅₀	0.059 × 10^-3μM Compound: 8, PXD101	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 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	[PMID: 25113875]
RAW264.7	IC₅₀	0.059 x 10^-3μM Compound: 8, PXD101	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 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	[PMID: 25113875]
RAW264.7	IC₅₀	2.2 μM Compound: 8, PXD101	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 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	[PMID: 25113875]
RAW264.7	IC₅₀	4.7 μM Compound: 8, PXD101	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 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	[PMID: 25113875]
RAW264.7	IC₅₀	8.28 μM Compound: 8, PXD101	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 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	[PMID: 25113875]
SAOS-2	GI₅₀	3.3 μM Compound: 54; PDX-101	Antiproliferative activity against human SAOS-2 cells Antiproliferative activity against human SAOS-2 cells	[PMID: 37875056]
SW-620	IC₅₀	2.53 μM Compound: 54; PDX-101	Antiproliferative activity against human SW620 cells incubated for 48 hrs by colorimetric method Antiproliferative activity against human SW620 cells incubated for 48 hrs by colorimetric method	[PMID: 37875056]
THP-1	GI₅₀	0.075 μM Compound: 2	Growth inhibition of human THP-1 cells Growth inhibition of human THP-1 cells	[PMID: 37429084]
THP-1	IC₅₀	0.4 μM Compound: Belinostat	Inhibition of cell growth of human THP-1 cells Inhibition of cell growth of human THP-1 cells	[PMID: 38236416]
U-937	IC₅₀	0.4 μM Compound: PXD101	Antiproliferative activity against human U937 cells after 48 hrs by MTT assay Antiproliferative activity against human U937 cells after 48 hrs by MTT assay	[PMID: 30879863]

In Vitro

Belinostat (PXD101) induces a concentration-dependent (0.2-5 μM) increase in acetylation of histone H4 in tumor cell lines. Belinostat is cytotoxic in vitro in a number of tumor cell lines with IC₅₀s in the range 0.2-3.4 μM as determined by a clonogenic assay and induces apoptosis. Belinostat inhibits the growth of a number of human tumor cell lines in vitro with IC₅₀s determined by a clonogenic assay in the range 0.2-3.4 μM^[1]. Belinostat (PXD101) is a potent histone deacetylase (HDAC) inhibitor, potently inhibits the enzymatic activity of purified recombinant HDAC6 (IC₅₀ of 82 nM)^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Solvente y solubilidad

In Vitro:

DMSO : 100 mg/mL (314.12 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : 25 mg/mL (78.53 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.1412 mL	15.7060 mL	31.4120 mL
5 mM	0.6282 mL	3.1412 mL	6.2824 mL
10 mM	0.3141 mL	1.5706 mL	3.1412 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.85 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 2

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (6.53 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (6.53 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

Pureza y Documentación

Purity: 99.97%

Ficha de datos (279 KB) SDS (396 KB)

COA (246 KB) HNMR (184 KB) RP-HPLC (257 KB) MS (69 KB) Elemental Analysis Report (104 KB)

Instrucciones de manejo (2659 KB)

Referencias

[1]. Plumb JA, et al. Pharmacodynamic response and inhibition of growth of human tumor xenografts by the novel histonedeacetylase inhibitor PXD101. Mol Cancer Ther. 2003 Aug;2(8):721-8. [Content Brief]

[2]. Qian X, et al. Activity of PXD101, a histone deacetylase inhibitor, in preclinical ovarian cancer studies. Mol Cancer Ther. 2006 Aug;5(8):2086-95. [Content Brief]

[3]. Chia S, et al. Phenotype-driven precision oncology as a guide for clinical decisions one patient at a time. Nat Commun. 2017 Sep 5;8(1):435. [Content Brief]

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Referencia HY-10225-10mg

Contact local distributor :

Marca : MedChemExpress

Contact local distributor :

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