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1mg |
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5mg |
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10mg |
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ln Vitro |
In all four lymphoma cell lines, alteminostat (CKD-581; 1 nM–10 μM; 72 hours) therapy significantly decreased cell viability in a concentration-dependent way. In SU-DHL-4, OCI-LY1, SU-DHL-2, and U2932 cells, the IC50 values of alteminostat are 1.31 nM, 36.91 nM, 1.18 nM, and 31.99 nM, respectively[1]. Cells treated with alteminostat (CKD-581; 10-300 nM; 24 hours) express less BCL-6 and BCL-2 [1]. In SU-DHL-4, OCI-LY1, SU-DHL-2, and U2932 cells, alteminostat (CKD-581; 30-300 nM; 24 hours) treatment causes γH2AX buildup and PARP1 cleavage. In OCI-LY1 cells, alteminostat decreases BCL-XL and MCL-1 protein levels in a concentration-dependent manner [1]. In SU-DHL-2 cells, alteminostat (CKD-581; 10-300 nM; 6 hours) treatment enhances histone H3 acetylation. Tubulin acetylation is similarly increased by 10 nM CKD-581. In lymphoma cells, CKD-581 inhibits class I–II HDACs, which leads to an increase in the acetylation of target molecules [1].
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ln Vivo |
SU-DHL-4 xenograft mice treated with alteminostat (CKD-581; 20–40 mg/kg; intraperitoneal injection; twice weekly; for 4 weeks) showed a partial but considerable reduction in tumor growth [1].
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Cell Assay |
Cell Viability Assay[1]
Cell Types: SU-DHL-4, OCI-LY1, SU-DHL-2 and U2932 Cell Tested Concentrations: 1 nM-10 μM Incubation Duration: 72 hrs (hours) Experimental Results: Cell viability of all four lymphomas Dramatically diminished cell lines in a concentration-dependent manner. Western Blot Analysis[1] Cell Types: SU-DHL-4 and OCI-LY1 Cell Tested Concentrations: 10 nM, 30 nM, 100 nM, 300 nM Incubation Duration: 24 hrs (hours) Experimental Results: diminished expression of BCL-6 and BCL-2 in in cells. |
Animal Protocol |
Animal/Disease Models: Male NOD.CB17 SCID injection of SU-DHL-4 cells [1]
Doses: 20 mg/kg or 40 mg/kg Route of Administration: intraperitoneal (ip) injection; twice a week; for 4 weeks Experimental Results: Partial but significant Inhibit tumor growth. |
References | |
Additional Infomation |
Alteminostat is a highly water-soluble, pan histone deacetylase (HDAC) inhibitor, with potential antineoplastic activity. Upon administration, alteminostat targets and inhibits HDAC, resulting in an accumulation of highly acetylated histones, the induction of chromatin remodeling, and an altered pattern of gene expression. This leads to the inhibition of tumor oncogene transcription, and the selective transcription of tumor suppressor genes, which results in the inhibition of tumor cell division and the induction of tumor cell apoptosis. HDACs, upregulated in many tumor cell types, are a family of metalloenzymes responsible for the deacetylation of chromatin histone proteins.
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Molecular Formula |
C27H36N6O3
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Molecular Weight |
492.613145828247
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Exact Mass |
492.284
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CAS # |
1246374-97-9
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PubChem CID |
58074180
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Appearance |
White to off-white solid powder
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Density |
1.2±0.1 g/cm3
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Index of Refraction |
1.631
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LogP |
2.89
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Hydrogen Bond Donor Count |
2
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Hydrogen Bond Acceptor Count |
5
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Rotatable Bond Count |
9
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Heavy Atom Count |
36
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Complexity |
708
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Defined Atom Stereocenter Count |
0
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InChi Key |
YEQGPOVCXMZUBT-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C27H36N6O3/c1-30-15-17-32(18-16-30)27(35)33(14-6-4-3-5-7-26(34)29-36)24-12-10-21(11-13-24)22-8-9-23-20-28-31(2)25(23)19-22/h8-13,19-20,36H,3-7,14-18H2,1-2H3,(H,29,34)
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Chemical Name |
N-[7-(hydroxyamino)-7-oxoheptyl]-4-methyl-N-[4-(1-methylindazol-6-yl)phenyl]piperazine-1-carboxamide
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO : ~230 mg/mL (~466.90 mM)
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.0300 mL | 10.1500 mL | 20.3000 mL | |
5 mM | 0.4060 mL | 2.0300 mL | 4.0600 mL | |
10 mM | 0.2030 mL | 1.0150 mL | 2.0300 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.