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| ln Vitro |
Various NIH3T3-derived transformed cell lines exhibit morphological reversal and junD transcriptional activation upon exposure to oxamflatin. When applied to several tumor cell lines from mice and humans, oxamflatin has antiproliferative activity and significantly alters the shape of the cells. HeLa cells that are exposed to olefantine undergo morphological elongation and filamentous protrusions, as well as a G1 phase cell cycle arrest. In a dose-dependent manner, oxamflatin significantly increases the transcriptional activity of the CMV promoter and suppresses intracellular HDAC activity [1]. OVCAR-5 and SKOV-3 ovarian cancer cell lines undergo morphological alterations when exposed to oxamflatin at nanomolar concentrations. Additionally, oxaxanthin treatment reduced the vitality of the cells. Cell division and DNA synthesis can be strongly inhibited by oxamflatin [2]. In the MKN-45 cell line, oxamflatin can decrease cell viability and promote the expression of E-cadherin [3].
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| ln Vivo |
Oxapine injections six times at a dose of 20 mg/kg resulted in a considerable increase in survival days (38 percent of ILS). One mouse lived for more than 60 days following tumor inoculation, while mice given oxamamine at a dose of 50 mg/kg were found to have an ILS of more than 67%. There were no negative consequences, such as weight loss, at least not at this dosage [1].
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| References |
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| Additional Infomation |
5-[3-(benzenesulfonamido)phenyl]-N-hydroxypent-2-en-4-ynamide is a sulfonamide.
Oxamflatin is an inhibitor of histone deacetylase. It is an aromatic sulfonamide hydroxamate initially found in a screen for inhibitors of the tumorigenic phenotype of K-ras-transformed NIH3T3 cells. |
| Molecular Formula |
C17H14N2O4S
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|---|---|
| Molecular Weight |
342.36906
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| Exact Mass |
342.067
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| CAS # |
151720-43-3
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| PubChem CID |
5353852
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.4±0.1 g/cm3
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| Index of Refraction |
1.686
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| LogP |
3.26
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
24
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| Complexity |
618
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC=C(C=C1)S(=O)(=O)NC2=CC=CC(=C2)C#C/C=C/C(=O)NO
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| InChi Key |
QRPSQQUYPMFERG-LFYBBSHMSA-N
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| InChi Code |
InChI=1S/C17H14N2O4S/c20-17(18-21)12-5-4-7-14-8-6-9-15(13-14)19-24(22,23)16-10-2-1-3-11-16/h1-3,5-6,8-13,19,21H,(H,18,20)/b12-5+
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| Chemical Name |
(E)-5-[3-(benzenesulfonamido)phenyl]-N-hydroxypent-2-en-4-ynamide
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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 |
| 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 : ~50 mg/mL (~146.04 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.30 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. Solubility in Formulation 2: ≥ 2.08 mg/mL (6.08 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 (6.08 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9208 mL | 14.6041 mL | 29.2082 mL | |
| 5 mM | 0.5842 mL | 2.9208 mL | 5.8416 mL | |
| 10 mM | 0.2921 mL | 1.4604 mL | 2.9208 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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