| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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| Targets |
HDAC6 82 nM (IC50) HDAC 27 nM (IC50, Hela cell)
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| ln Vitro |
In tumor cell lines, belinostat (PXD101) causes an increase in the acetylation of histone H4 that is concentration-dependent (0.2–5 μM). A clonogenic study revealed that belinostat is cytotoxic in vitro in a variety of tumor cell lines, causing apoptosis with IC50s in the 0.2–3.4 μM range. Many human tumor cell lines are inhibited in vitro by belinostat, whose IC50s, as measured by a clonogenic experiment, fall between 0.2 and 3.4 μM[1]. The enzymatic activity of pure recombinant HDAC6 (IC50 of 82 nM) is potently inhibited by belinostat (PXD101), a strong histone deacetylase (HDAC) inhibitor[2].
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| ln Vivo |
For seven days, Belinostat (10–40 mg/kg/day ip) was given intraperitoneally to nude mice carrying human ovarian and colon tumor xenografts. This treatment significantly delayed the animals's growth without showing any overt evidence of harm. Cells resistant to cisplatin found in ovarian tumor xenografts also show growth retardation. Three hours following treatment with belinostat (PXD101), a significant rise in acetylation of H4 is found in the blood and tumor of mice. mice's human tumor xenografts are grown less rapidly, and there is no visible toxicity[1]. When used in combination with carboplatin therapy, belinostat (PXD101) exhibits increased single-agent antitumor efficacy on human A2780 ovarian cancer sc xenografts[2].
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| References |
[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.
[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. [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 |
| Molecular Formula |
C15H14N2O4S
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|---|---|
| Molecular Weight |
318.35
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| CAS # |
866323-14-0
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| Related CAS # |
866323-14-0; 414864-00-9;
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| SMILES |
S(C1=C([H])C([H])=C([H])C(/C(/[H])=C(\[H])/C(N([H])O[H])=O)=C1[H])(N([H])C1C([H])=C([H])C([H])=C([H])C=1[H])(=O)=O
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| Solubility (In Vitro) |
DMSO : 100 mg/mL (314.12 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.85 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (6.53 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (6.53 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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