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| Targets |
Caspase 3
Raptinal targets the intrinsic apoptotic pathway, specifically promoting the release of cytochrome c from the mitochondria. It directly activates caspase-3, bypassing the activation of promoter caspase-8 and caspase-9. By activating the mitochondrial pathway-mediated intrinsic apoptosis, Raptinal induces rapid cancer cell death. The compound is hydrolyzed into its active form in aqueous solutions. |
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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].
In vitro, Raptinal (10 µM) induces apoptosis in 17 cancerous and non-cancerous cell lines including HFF-1 IRR, MCF-10A, MEFs, and 3T3-SA cells. It shows complete cytochrome c release within 30 minutes and caspase-3 activation within one hour of exposure at 10 µM. Raptinal directly activates caspase-3 and can initiate the caspase-dependent intrinsic pathway of apoptosis. It rapidly induces cancer cell death by directly activating effector caspase-3, bypassing promoter caspase-8 and caspase-9 activation. |
| 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].
In vivo, Raptinal (20 mg/kg per day) decreases tumor mass in a 4T1 murine breast cancer model. This demonstrates its potential as an anticancer agent in preclinical models. The compound's ability to directly activate the intrinsic apoptotic pathway makes it a valuable tool for studying apoptosis and developing cancer therapies. However, specific published in vivo protocols are not detailed in the available literature. |
| Enzyme Assay |
The in vitro apoptosis assay for Raptinal is conducted in various cell lines including cancer cells and non-cancerous cells such as HFF-1 IRR, MCF-10A, MEFs, and 3T3-SA. Cells are treated with Raptinal at 10 µM. Apoptosis is measured by flow cytometry using Annexin V/PI staining, caspase activity assays, and detection of cytochrome c release and DNA fragmentation. Cytochrome c release is measured within 30 minutes, and caspase-3 activation is assessed within one hour.
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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. Cellular assays for Raptinal are conducted in cancer cell lines and non-cancerous cell lines. Cells are treated with varying concentrations of Raptinal (typically 10 µM). Apoptosis is assessed by flow cytometry using Annexin V/PI staining, caspase activity assays, and detection of cytochrome c release. The compound's effects on cell viability and proliferation are measured using standard assays such as MTT or CellTiter-Glo. The rapid kinetics of apoptosis induction are confirmed by time-course experiments showing cytochrome c release within 30 minutes and caspase-3 activation within one hour. |
| 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. In vivo studies for Raptinal are conducted in a 4T1 murine breast cancer model. The compound is administered at 20 mg/kg per day. Efficacy is assessed by measuring tumor mass reduction. Pharmacodynamic markers such as apoptosis are evaluated in tumor tissues. However, specific published in vivo protocols for Raptinal are not detailed in the available literature. The compound is currently used as a research tool for studying apoptosis and cancer therapeutics. |
| ADME/Pharmacokinetics |
Pharmacokinetic data for Raptinal is not extensively reported in publicly available sources. The compound has a molecular weight of 386.4 g/mol and a molecular formula of C28H18O2. It is slightly soluble in DMSO, ethanol, and PBS (pH 7.2). Storage conditions: -20°C. As a small molecule apoptosis inducer, it is expected to have moderate bioavailability. Detailed PK parameters such as half-life are not available in the current literature.
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| Toxicity/Toxicokinetics |
In vivo, Raptinal (20 mg/kg per day) decreases tumor mass in a 4T1 murine breast cancer model. As with all research compounds, Raptinal is intended for research use only and not for human therapeutic applications. The compound's potent apoptosis-inducing activity suggests potential toxicity concerns that would need to be addressed. Standard in vitro cytotoxicity assays and in vivo tolerability studies would be required for a complete toxicity assessment.
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| References | |
| Additional Infomation |
Raptinal is a cell-permeable bifluorene-dicarbaldehyde compound that acts as a rapid activator of mitochondrial pathway-mediated intrinsic apoptosis. It directly activates caspase-3 and can initiate the caspase-dependent intrinsic pathway of apoptosis, bypassing promoter caspase-8 and caspase-9. Raptinal induces complete cytochrome c release within 30 minutes and caspase-3 activation within one hour at 10 µM. In vivo, Raptinal (20 mg/kg per day) decreases tumor mass in a 4T1 murine breast cancer model. It has a molecular formula of C28H18O2 and a molecular weight of 386.4 g/mol.
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| Molecular Formula |
C28H18O2
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|---|---|
| Molecular Weight |
386.44
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| Exact Mass |
386.131
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| CAS # |
1176-09-6
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| PubChem CID |
355994
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| Appearance |
White to off-white solid powder
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| Melting Point |
219 °C
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| LogP |
5.317
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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 |
3
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| Heavy Atom Count |
30
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| Complexity |
580
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
GLANOOJJBKXTMI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C28H18O2/c29-17-27(23-13-5-1-9-19(23)20-10-2-6-14-24(20)27)28(18-30)25-15-7-3-11-21(25)22-12-4-8-16-26(22)28/h1-18H
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| Chemical Name |
9-(9-formylfluoren-9-yl)fluorene-9-carbaldehyde
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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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