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| Targets |
Caspase 3
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| ln Vitro |
Gastric epithelial cells' apoptotic resistance brought on by H. Raptinal is the cause of pylori infection [1]. Pro-caspase-3 can be cleaved into the active form in human gastric cancer cell lines AGS, MKN28, and MKN45 when treated with 10 μM Raptinal for two hours [1]. In a matter of minutes, raptinal triggers apoptosis in several cell lines that is dependent on the caspase intrinsic route. Numerous cancer and non-cancer cell lines can be killed by raptinal, and its 24-hour IC50 value ranges from 0.7 to 3.4 μM, suggesting that it is effective against a wide range of cell lines [2].
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| ln Vivo |
In a variety of cell lines and in vivo settings, raptinal induces caspase-dependent apoptosis exceptionally quickly [1]. In vivo anticancer efficacy is exhibited by raptinal (20 mg/kg; intraperitoneally given; once daily for 3 days in the B16-F10 model and 4 days in the 4T1 animal) [2]. A single injection of Raptinal at various doses was administered to C57BL/6 mice. Raptinal's peak plasma concentration and elimination half-life were 54.4±0.9 μg/mL and 92.1±5.8 minutes, respectively, when it was given intravenously at a dose of 37.5 mg/kg. When evaluated seven days after treatment, single intravenous doses of Raptinal were well tolerated over a broad dose range (15–60 mg/kg) and did not result in hematological damage [2].
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| Cell Assay |
Cell Viability Assay[2]
Cell Types: Human Lymphoma U-937, SKW 6.4, or Jurkat cell lines Tested Concentrations: 0.7-3.4 μM Incubation Duration: 24 hrs (hours) Experimental Results: The IC50 values of Raptinal against U-937, SKW 6.4, or Jurkat cell lines were 1.1±0.1, 0.7±0.3, 2.7±0.9 μM, respectively. Western Blot Analysis[1] Cell Types: Human gastric cancer cell lines AGS, MKN28, MKN45 Tested Concentrations: 10 μM Incubation Duration: 2 hrs (hours) Experimental Results: Induced apoptosis by activating caspase-3 within 30 min at a concentration of 10 μM. Treatment with 10 μM of Raptinal for 2 h induced the cleavage of pro -caspase-3 into it's active form in all three cell lines. |
| Animal Protocol |
Animal/Disease Models: C57BL/6 and BALB/c female mice (6-8 weeks old) bearing the B16-F10 model or 4T1 models[2]
Doses: 20 mg/kg Route of Administration: Administered intraperitoneally (ip); one time/day for 3 days for B16-F10 and 4 days for 4T1 models Experimental Results: Retard tumor volume and tumor mass by 60% relative to controls in the B16-F10 model. Similar efficacy was observed for the 4T1 murine breast cancer tumor model with 50% growth inhibition after treatment. |
| References |
[1]. Yanheng Chen, et al. H. pylori infection confers resistance to apoptosis via Brd4-dependent BIRC3 eRNA synthesis. Cell Death Dis. 2020 Aug 21;11(8):667.
[2]. Rahul Palchaudhuri,et al. A Small Molecule that Induces Intrinsic Pathway Apoptosis with Unparalleled Speed. Cell Rep. 2015 Dec 1;13(9):2027-36. |
| Molecular Formula |
C28H18O2
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|---|---|
| Molecular Weight |
386.44
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| CAS # |
1176-09-6
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| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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| SMILES |
O=CC1(C2C=CC=CC=2C2=CC=CC=C12)C1(C=O)C2C=CC=CC=2C2=CC=CC=C12
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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 : 20 mg/mL (51.75 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.47 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 25.0 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: ≥ 2.5 mg/mL (6.47 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5877 mL | 12.9386 mL | 25.8772 mL | |
| 5 mM | 0.5175 mL | 2.5877 mL | 5.1754 mL | |
| 10 mM | 0.2588 mL | 1.2939 mL | 2.5877 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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