| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg | |||
| 50mg | |||
| Other Sizes |
| Targets |
SR-11302 targets activator protein-1 (AP-1), a transcription factor composed of Jun, Fos, and ATF proteins that regulates genes involved in cell proliferation, differentiation, and apoptosis. SR-11302 inhibits AP-1 activity without activating retinoic acid response elements, making it a specific AP-1 inhibitor. By targeting AP-1, SR-11302 exhibits potential anti-inflammatory and anticancer properties.
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| ln Vitro |
Strong anti-AP-1 activity is exhibited by SR 11302 (SR11302), which selectively binds to RARα and RARγ but not to RARβ or RXRα [1]. In cells treated with hypoxia, SR 11302 (SR-11302; 1 μM) decreases aldosterone levels by 61.9% and inhibits the activity of the AP-1 transcription factor [2]. Helicobacter pylori (H. pylori)-induced gastric adenocarcinoma (AGS) cell proliferation is inhibited by SR 11302 (SR-11302; 2 μM; 48 hours) [3]. In AGS cells, β-catenin and c-myc expression generated by Helicobacter pylori is inhibited by SR 11302 (2 μM; 24 hours) [3].
In vitro, SR-11302 can inhibit the growth of breast cancer cell line T-47D, the lung cancer line Calu-6, and HeLa cells. SR-11302 (1 µM) reduces metastatic lesion formation in a 4D lung cancer model. Analysis of tumor cells grown on an ex vivo 4D lung cancer model shows an increase in components of AP-1, c-Fos and c-Jun, in circulating tumor cells (CTC) compared to primary tumor. |
| ln Vivo |
Treatment with SR 11302 (SR11302; low dosage 0.5 mg/kg and high dose 1 mg/kg body weight; daily oral gavage) lowers total vascular lesion number and lesion size in Vldlr-/- mice in a dose-dependent manner [4] .
In vivo activity data for SR-11302 are not extensively detailed in the available sources. The compound is under investigation for its therapeutic implications in various diseases and conditions. Its ability to inhibit AP-1 suggests potential applications in cancer and inflammatory diseases, but specific in vivo efficacy data in animal models have not been reported in the supplier documentation. |
| Enzyme Assay |
The in vitro assay for SR-11302 involves measuring its inhibition of AP-1 transcriptional activity. Cell-based reporter assays are typically used, where cells are transfected with a luciferase reporter construct containing AP-1 binding sites. Cells are treated with SR-11302 at varying concentrations, and AP-1 activity is quantified by measuring luciferase activity. The compound's ability to inhibit AP-1-mediated transcription is determined from dose-response curves.
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| Cell Assay |
Cellular assays for SR-11302 are performed using cancer cell lines such as T-47D (breast cancer), Calu-6 (lung cancer), and HeLa cells. Cells are treated with SR-11302 at various concentrations (e.g., 1 µM). Cell proliferation and viability are assessed using standard assays such as MTT or CellTiter-Glo. Metastatic lesion formation is evaluated in 4D lung cancer models.
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| Animal Protocol |
Animal/Disease Models: Vldlr-/- mice [4]
Doses: low dose 0.5 mg/kg and high dose 1 mg/kg Body weight Route of Administration: P5 to P15 Daily po (oral gavage) Experimental Results: P5 to P15 High dose reduces total vascular lesions The number was diminished by 48%, the lesion size was diminished by 40%, and no signs of toxicity were detected in the mice, including no changes in body weight. In vivo animal studies for SR-11302 are not detailed in the available sources. The compound has been investigated in ex vivo 4D lung cancer models, where it reduces metastatic lesion formation. Specific animal models, dosing regimens, and efficacy data have not been reported in the supplier documentation. |
| ADME/Pharmacokinetics |
Pharmacokinetic data for SR-11302 are not available in the provided sources. The compound has a molecular weight of 376.53 g/mol and a molecular formula of C26H32O2. It is soluble to 100 mM in DMSO and to 10 mM in ethanol. The compound should be stored at -20°C.
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| Toxicity/Toxicokinetics |
Toxicity data for SR-11302 are not reported in the available sources. As a research compound, it is not intended for therapeutic use. The compound has been evaluated in cell-based assays at concentrations up to 1 µM without significant toxicity reported. Specific toxicological profiles have not been characterized.
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| References |
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| Additional Infomation |
SR11302 is a retinoid compound with the structure all-trans retinoic acid, wherein the methyl group at position 9 is replaced by a 4-methylphenyl group. It is an activator protein-1 (AP-1) inhibitor with antitumor activity in vivo. It can function as an AP-1 antagonist and an antitumor drug. SR11302 belongs to the retinoid class of compounds, is a toluene derivative, and is an α,β-unsaturated monocarboxylic acid. Its function is related to all-trans retinoic acid.
SR-11302 is a research compound for studying AP-1 function in cancer and inflammation. It is a synthetic retinoid that specifically inhibits AP-1 without activating retinoic acid response elements. The compound is available from commercial suppliers for research use only. A reference publication describing its use is available (Mishra DK, Kim MP, 2017). |
| Molecular Formula |
C26H32O2
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|---|---|
| Molecular Weight |
376.53108
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| Exact Mass |
376.24
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| CAS # |
160162-42-5
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| Related CAS # |
(6E)-SR 11302
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| PubChem CID |
9976842
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.048g/cm3
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| Boiling Point |
541.567ºC at 760 mmHg
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| Flash Point |
414.977ºC
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| Vapour Pressure |
0mmHg at 25°C
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| Index of Refraction |
1.587
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| LogP |
7.048
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
28
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| Complexity |
705
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=C(C(CCC1)(C)C)/C=C/C(=C/C=C/C(=C/C(=O)O)/C)/C2=CC=C(C=C2)C
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| InChi Key |
RQANARBNMTXCDM-DKOHIBGUSA-N
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| InChi Code |
InChI=1S/C26H32O2/c1-19-11-13-23(14-12-19)22(10-6-8-20(2)18-25(27)28)15-16-24-21(3)9-7-17-26(24,4)5/h6,8,10-16,18H,7,9,17H2,1-5H3,(H,27,28)/b8-6+,16-15+,20-18+,22-10-
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| Chemical Name |
(2E,4E,6Z,8E)-3-methyl-7-(4-methylphenyl)-9-(2,6,6-trimethylcyclohexen-1-yl)nona-2,4,6,8-tetraenoic acid
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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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 : ~25 mg/mL (~66.40 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (6.64 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 sonication.
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 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. Solubility in Formulation 2: 2 mg/mL (5.31 mM) in 1% CMC-Na/saline water (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O 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 | 2.6558 mL | 13.2792 mL | 26.5583 mL | |
| 5 mM | 0.5312 mL | 2.6558 mL | 5.3117 mL | |
| 10 mM | 0.2656 mL | 1.3279 mL | 2.6558 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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