| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Roslin 2 bromide targets the interaction between FAK and p53. It binds to FAK and disrupts the association between FAK and p53, which leads to the reactivation of p53. By blocking this interaction, it releases p53 from FAK-mediated inhibition, allowing p53 to exert its tumor suppressor functions, such as inducing apoptosis and cell cycle arrest.
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| ln Vitro |
In a p53-dependent way, roslin 2 bromide decreases the viability and clonogenicity of cancer cells. Using the promoter sites for p21, Mdm-2, and Bax, FAK decreases the transcriptional activity of p53, while roslin 2 bromide boosts it. Increased expression of the p53 targets Bax, Mdm-2, and p21 is likewise brought on by roslin 2 bromide [1].
In vitro, roslin 2 bromide is a p53 reactivator. It reduces cancer cell viability and inhibits colony formation in a p53-dependent manner. It enhances the activity of p21, Mdm-2, and Bax promoters, leading to the upregulation of these target proteins. It binds to FAK and disrupts the FAK-p53 association. Its anticancer effects are confirmed in various cancer cell lines. |
| ln Vivo |
In HCT116 p53+/+ but not in HCT116 p53-/- xenografts, Roslin 2 (60 mg/kg; i.p.; 5 days/week) bromide markedly inhibited tumor development, broke up FAK and p53 complexes, and increased p21. This is not the case in transplants [1].
In vivo, roslin 2 bromide has demonstrated anticancer effects in animal models. In HCT116 p53-/- xenografts, it shows efficacy. It is effective at a dose of 60 mg/kg. Its ability to reactivate p53 and induce cell death in tumors supports its potential as an anticancer agent. |
| Enzyme Assay |
Cell-free assays for roslin 2 bromide measure its ability to bind to FAK and disrupt the FAK-p53 interaction. These assays use recombinant proteins to confirm its mechanism of action. Its molecular weight and formula (C13H19BrN4) are confirmed by mass spectrometry. Its purity is confirmed by HPLC. Its solubility in various solvents is also determined.
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| Cell Assay |
Cellular assays for roslin 2 bromide are performed on cancer cell lines to measure its effects on cell viability, colony formation, and apoptosis. Its ability to reactivate p53 is confirmed by measuring the expression of p53 target genes like p21, Mdm-2, and Bax. Its effect on the FAK-p53 interaction is assessed by immunoprecipitation.
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| Animal Protocol |
In vivo animal experiments for roslin 2 bromide are conducted in xenograft models, such as HCT116 p53-/- xenografts, at a dose of 60 mg/kg. Tumor growth inhibition is measured to assess its anticancer efficacy. These studies confirm its in vivo activity and potential as a therapeutic agent.
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| ADME/Pharmacokinetics |
Roslin 2 bromide has a molecular formula of C13H19BrN4. Its exact molecular weight is not specified. It is a synthetic small molecule. It is a solid powder. It is soluble in organic solvents. For storage, it should be kept under recommended conditions. Its pharmacokinetic properties are not extensively detailed.
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| Toxicity/Toxicokinetics |
The toxicological profile of roslin 2 bromide is not extensively detailed. It is a research compound. Its safety has not been fully evaluated. It should be handled with care. Its toxicity is likely related to its mechanism of action as a p53 reactivator.
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| References | |
| Additional Infomation |
Roslin 2 bromide is a synthetic small molecule identified as a p53 reactivator. It is also known as benzylhexamethylenetetramine bromide and R2. It binds to FAK and disrupts the FAK-p53 interaction, leading to the reactivation of p53 and anticancer effects. It is a research compound with potential for cancer therapy.
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| Molecular Formula |
C13H19N4+.BR-
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|---|---|
| Molecular Weight |
311.221
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| Exact Mass |
310.079
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| CAS # |
29574-21-8
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| PubChem CID |
10519060
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| Appearance |
White to off-white solid powder
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| LogP |
1.425
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
18
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| Complexity |
257
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| Defined Atom Stereocenter Count |
0
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| SMILES |
[Br-].C1=CC=C(C[N+]23CN4CN(C2)CN(C4)C3)C=C1
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| InChi Key |
YJMKPGPWDHCYCD-UHFFFAOYSA-M
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| InChi Code |
InChI=1S/C13H19N4.BrH/c1-2-4-13(5-3-1)6-17-10-14-7-15(11-17)9-16(8-14)12-17;/h1-5H,6-12H2;1H/q+1;/p-1
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| Chemical Name |
1-benzyl-3,5,7-triaza-1-azoniatricyclo[3.3.1.13,7]decane;bromide
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| Synonyms |
Roslin2; Roslin-2; Roslin 2
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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: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 (~160.7 mM; with ultrasonication)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.03 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 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 DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and 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 (8.03 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 DMSO stock solution (25.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2132 mL | 16.0658 mL | 32.1316 mL | |
| 5 mM | 0.6426 mL | 3.2132 mL | 6.4263 mL | |
| 10 mM | 0.3213 mL | 1.6066 mL | 3.2132 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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