| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
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Purity: ≥98%
Splitomicin (known also as Splitomycin), a lactone derived from naphthol, is a potent, cell-permeable and selective inhibitor of NAD(+)-dependent histone deacetylase (HDAC) Sir2p with potential antineoplastic activity. It inhibits Sir2p with an IC50 of 60 μM. Splitomicin was discovered for yeast sirtuins but showed rather weak inhibition on human enzymes.
| ln Vitro |
MCF-7 and H1299 cells are treated with splitomicin (10-333 μM) for 24 hours, and the antiproliferative impact is concentration-dependent. Splitomicin effectively suppresses MCF-7 and H1299 cell colony formation at 100 and 333 μM, but it is unable to decrease the number of colonies at 33 μM [2].
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| ln Vivo |
Splitomicin increases tissue factor (TF) activity in the arterial vessel wall and speeds up carotid artery thrombosis in C57BL/6 mice when given intraperitoneally every 24 hours for five days at a dose of 80 mg/kg [3].
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| Cell Assay |
Cell Proliferation Assay[2]
Cell Types: Human breast cancer MCF-7 and lung cancer H1299 cells Tested Concentrations: 10, 33, 100, and 333 μM Incubation Duration: 24 hrs (hours) Experimental Results: Inhibited colony formation in a dose-dependent manner. |
| Animal Protocol |
Animal/Disease Models: C57BL/6 mice aged 12-14 weeks weighing on average 27 g[3]
Doses: 80 mg/kg Route of Administration: intraperitoneal (ip)injection every 24 h for 5 days Experimental Results: Increased TF activity in mouse carotid artery as compared with the controls . |
| References |
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| Additional Infomation |
Splitomicin is a benzochromenone that is 2,3-dihydro-1H-benzo[f]chromene substituted by an oxo group at position 3. It has been found to exhibit potential inhibitory activity against Sir2 proteins. It has a role as a Sir2 inhibitor and a platelet aggregation inhibitor. It is a benzochromenone, a delta-lactone and a naphtho-alpha-pyrone.
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| Molecular Formula |
C13H10O2
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|---|---|---|
| Molecular Weight |
198.22
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| Exact Mass |
198.068
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| CAS # |
5690-03-9
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| Related CAS # |
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| PubChem CID |
5269
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| Appearance |
White to light yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
383.6±17.0 °C at 760 mmHg
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| Melting Point |
73-74.5℃
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| Flash Point |
161.2±18.4 °C
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| Vapour Pressure |
0.0±0.9 mmHg at 25°C
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| Index of Refraction |
1.656
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| LogP |
3.03
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
15
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| Complexity |
261
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
ISFPDBUKMJDAJH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H10O2/c14-13-8-6-11-10-4-2-1-3-9(10)5-7-12(11)15-13/h1-5,7H,6,8H2
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| Chemical Name |
1H-benzo[f]chromen-3(2H)-one
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| Synonyms |
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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 |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (10.49 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 (10.49 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 (10.49 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 | 5.0449 mL | 25.2245 mL | 50.4490 mL | |
| 5 mM | 1.0090 mL | 5.0449 mL | 10.0898 mL | |
| 10 mM | 0.5045 mL | 2.5224 mL | 5.0449 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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