BMS 453 (Synonyms: BMS 189453) |
Catalog No.GC10656
One-Click Copy Product Info
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RAR agonist
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 166977-43-1
Sample solution is provided at 25 µL, 10mM.
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BMS 453 is a synthetic RAR (retinoic acid receptor) antagonist [1].
The retinoic acid receptors (RARα, RARβ, RARγ) belong to steroid nuclear receptor superfamily and the expressions of retinoid receptor RARα and RARβ are correlated with the antiproliferative effects of retinoids.
In normal breast cells, BMS453 inhibited the cell proliferation without significantly apoptosis. BMS 453 blocked the G1/S transition of the cell cycle with an increase in the amount of cells in G0/G1 and a decrease in the amount of cells in S phase. Also, BMS453 increased active TGFβ activity by 33-fold, which show BMS453 induces conversion of latent TGFβ to active TGFβ. TGFβ mediates the anti-proliferative effect of BMS453 in breast cells [1]. BMS 453 transrepresses AP-1 but does not activate RAR-dependent gene expression. In normal breast cells (HMEC and 184) and T47D breast cancer cells, BMS453 inhibited the growth of T47D breast cancer cells and normal breast cells (HMEC and 184). Breast cancer cells were resistant to BMS453 and normal human breast cells were most sensitive to BMS453. BMS453 may suppress growth by inhibiting transcription factors such as AP-1 [2].
References:
[1]. Yang L, Ostrowski J, Reczek P, et al. The retinoic acid receptor antagonist, BMS453, inhibits normal breast cell growth by inducing active TGFbeta and causing cell cycle arrest. Oncogene, 2001, 20(55): 8025-8035.
[2]. Yang L, Munoz-Medellin D, Kim HT, et al. Retinoic acid receptor antagonist BMS453 inhibits the growth of normal and malignant breast cells without activating RAR-dependent gene expression. Breast Cancer Res Treat, 1999, 56(3): 277-291.
| Cas No. | 166977-43-1 | SDF | |
| Synonyms | BMS 189453 | ||
| Chemical Name | (E)-4-(2-(5,5-dimethyl-8-phenyl-5,6-dihydronaphthalen-2-yl)vinyl)benzoic acid | ||
| Canonical SMILES | OC(C1=CC=C(C=C1)/C=C/C2=CC=C3C(C)(C)CC=C(C4=CC=CC=C4)C3=C2)=O | ||
| Formula | C27H24O2 | M.Wt | 380.48 |
| Solubility | DMF: 5 mg/ml,DMSO: 10 mg/ml | 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 | 2.6283 mL | 13.1413 mL | 26.2826 mL |
| 5 mM | 525.7 μL | 2.6283 mL | 5.2565 mL |
| 10 mM | 262.8 μL | 1.3141 mL | 2.6283 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 saline, 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: >98.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 16 reference(s) in Google Scholar.)