| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
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| Targets |
HDAC1 0.11 nM (IC50) HDAC2 0.33 nM (IC50) HDAC11 0.37 nM (IC50) HDAC10 0.46 nM (IC50) HDAC5 3.69 nM (IC50) HDAC8 4.26 nM (IC50) HDAC3 4.86 nM (IC50) HDAC9 32.1 nM (IC50) HDAC6 76.8 nM (IC50) HDAC7 119 nM (IC50)
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|---|---|
| ln Vitro |
In vitro, JNJ-26481585 suppresses HDAC isozymes[1]. In tumor cells, JNJ-26481585 (30–1000 nM; 24 hours) is a strong pan-HDAC inhibitor[1]. JNJ-26481585 causes apoptosis and exhibits broad spectrum antiproliferative action against hematologic and solid cancer cell lines[1].
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| ln Vivo |
p21waf1,cip1 ZsGreen tumors in vivo with JNJ-26481585 (40 mg/kg; po; once daily, for 3 days) as a strong HDAC1 inhibitor[1]. In vivo, JNJ-26481585 consistently causes H3 acetylation in tumor tissue[1]. Large pre-established HCT116 colon xenografts are vigorously inhibited in their growth by JNJ-26481585 (10 mg/kg; once daily; ip; for 14 days)[1].
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: Human A2780 ovarian carcinoma cells Tested Concentrations: 30 nM, 100 nM, 300 nM, 1000 nM Incubation Duration: 24 hrs (hours) Experimental Results: Induced H3 and H4 acetylation at concentrations as low as 30 to 100 nM. |
| Animal Protocol |
Animal/Disease Models: NMRI nude mice, with HCT116 colon carcinoma cells xenografts[1]
Doses: 10 mg/kg Route of Administration: intraperitoneal (ip)injection, one time/day, for 14 days Experimental Results: Strongly inhibited the growth of large pre-established HCT116 colon xenografts. |
| References |
[1]. Arts J, et al. JNJ-26481585, a novel "second-generation" oral histone deacetylase inhibitor, shows broad-spectrum preclinical antitumoral activity. Clin Cancer Res. 2009 Nov 15;15(22):6841-51.
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| Molecular Formula |
C21H28CL2N6O2
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|---|---|
| Molecular Weight |
467.39
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| CAS # |
875320-31-3
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| Related CAS # |
Quisinostat;875320-29-9
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| SMILES |
Cl[H].Cl[H].O=C(C1C([H])=NC(=NC=1[H])N1C([H])([H])C([H])([H])C([H])(C([H])([H])N([H])C([H])([H])C2=C([H])N(C([H])([H])[H])C3=C([H])C([H])=C([H])C([H])=C23)C([H])([H])C1([H])[H])N([H])O[H]
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| Solubility (In Vitro) |
DMSO : 31.25 mg/mL (66.86 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.45 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. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.45 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 20.8 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.45 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 | 2.1395 mL | 10.6977 mL | 21.3954 mL | |
| 5 mM | 0.4279 mL | 2.1395 mL | 4.2791 mL | |
| 10 mM | 0.2140 mL | 1.0698 mL | 2.1395 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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