SR 11302 |
| Catalog No.GC12810 |
An inhibitor of retinoid-induced AP-1 signaling
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 160162-42-5
Sample solution is provided at 25 µL, 10mM.
SR 11302 is an inhibitor of activator protein-1 (AP-1) [1].AP-1 is a transcription factor that displays antitumor effects in vivo.
SR 11302 is an inhibitor of AP-1 but don’t activate RARs and RXR. SR11302 failed to inhibit the proliferation of F9 cells, the embryonal carcinoma cell line. While, it can inhibit the growth of breast cancer cell line T-47D, the lung cancer line Calu-6 and HeLa cells[1]. SR 11302 had very little effect on either the proliferation or the differentiation of HL-60, fresh APL and NB4 cells, which indicate that AP-1 may not be involved in the signaling pathway of proliferation and differentiation of HL-60, fresh APL and NB4 cells [2].
In an AP-1-luciferase transgenic mouse carcinogenesis model, SR11302 significantly inhibit both AP-1 activation in 7,12-dimethyl benz(a)anthracene-initiated mouse skin and 12-O-tetradecanoylphorbol-13-acetate-induced papilloma formation. While, SR11235, a retinoid with RARE transactivating activity, but lack of AP-1 inhibiting effect, didn’t inhibit papilloma formation and AP-1 activation. These results show that the antitumor effect of retinoids is mediated by blocking AP-1 activity in vivo [3].
References:
[1]. Fanjul A, Dawson MI, Hobbs PD, et al. A new class of retinoids with selective inhibition of AP-1 inhibits proliferation. Nature, 1994, 372(6501): 107-111.
[2]. Shiohara M, Dawson MI, Hobbs PD, et al. Effects of novel RAR- and RXR-selective retinoids on myeloid leukemic proliferation and differentiation in vitro. Blood, 1999, 93(6): 2057-2066.
[3]. Huang C, Ma WY, Dawson MI, et al. Blocking activator protein-1 activity, but not activating retinoic acid response element, is required for the antitumor promotion effect of retinoic acid. Proc Natl Acad Sci U S A, 1997, 94(11): 5826-5830.
| Cell experiment [1]: | |
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Cell lines |
T-47D, Calu-6 and HeLa cell lines |
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Preparation method |
The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
10-6 M |
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Applications |
SR 11302 inhibits effectively the proliferation of T-47D, Calu-6 and HeLa cell lines, and could serve as a candidate for new retinoid therapeutic agent with reduced side effects. |
| Animal experiment [2]: | |
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Animal models |
AP-1-luciferase transgenic mice |
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Dosage form |
four times over 7 days with 34 nmol dissolved in 300 μl acetone |
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Application |
SR 11302 is one of the most promising drug candidate for chemotherapy and chemoprevention of cancer, and its effect is mediated by blocking AP-1 activity. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1] Fanjul A, Dawson MI, Hobbs PD, et al. A new class of retinoids with selective inhibition of AP-1 inhibits proliferation. Nature, 1994, 372(6501): 107-111. [2] Huang C, Ma WY, Dawson MI, et al. Blocking activator protein-1 activity, but not activating retinoic acid response element, is required for the antitumor promotion effect of retinoic acid. Proc Natl Acad Sci U S A, 1997, 94(11): 5826-5830. |
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| Cas No. | 160162-42-5 | SDF | |
| Chemical Name | 3-methyl-7-(4-methylphenyl)-9-(2,6,6-trimethylcyclohexen-1-yl)nona-2,4,6,8-tetraenoic acid | ||
| Canonical SMILES | CC1=C(C(CCC1)(C)C)C=CC(=CC=CC(=CC(=O)O)C)C2=CC=C(C=C2)C | ||
| Formula | C26H32O2 | M.Wt | 376.54 |
| Solubility | 0.5 mg/ml in ethanol; 10mg/ml in DMSO; 20mg/mL in DMF | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.6558 mL | 13.2788 mL | 26.5576 mL |
| 5 mM | 0.5312 mL | 2.6558 mL | 5.3115 mL |
| 10 mM | 0.2656 mL | 1.3279 mL | 2.6558 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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