| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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SR-11302 (SR11302) is an AP-1 (activator protein-1) transcription factor inhibitor with antitumor activity. SR11302 does not activate transcription from the retinoic acid response element (RARE) and displays no activity at retinoic acid receptors (EC50 > 1 μM for RARα, RARβ, RARγ and RXRα).
| 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].
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| 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] .
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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. |
| References |
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| Additional Infomation |
SR11302 is a retinoid that is all-trans-retinoic acid in which the methyl group at position 9 is replaced by a 4-methylphenyl group. It is an inhibitor of activator protein-1 which exhibits antitumour effects in vivo. It has a role as an AP-1 antagonist and an antineoplastic agent. It is a retinoid, a member of toluenes and an alpha,beta-unsaturated monocarboxylic acid. It is functionally related to an all-trans-retinoic acid.
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| 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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| 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 |
| 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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