AGN 194310 (Synonyms: VTP-194310) |
| Catalog No.GC12598 |
pan-RAR antagonist
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 229961-45-9
Sample solution is provided at 25 µL, 10mM.
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AGN 194310 is a pan-antagonist of retinoic acid receptors (RARs) with Kd values of 3nM, 2nM and 5nM for RAR α, RARβ and RARγ, respectively [1].
AGN 194310 has been reported to bind to RARs with equal and high Kd values of 3, 2 and 5nM for RAR α, RARβ and RARγ, respectively, by in vitro binding experiments. In addition, AGN 194310 has been revealed to potently inhibit the colony formation by ITS+-grown cell lines with IC50 values of 16 ± 5nM for LNCaP cells; 18 ± 6nM for PC3 cells; and 34 ± 7nM for DU-145 cells. Apart from these, because of binding to and mediating the effects via RARs, AGN 194310 has been demonstrated to inhibit agonist-induced (TTNPB) differentiation of HL60 cells. AGN 194310 has also shown the accumulation of cell in G1 and the function of induced apoptosis [1].
References:
[1] Hammond LA1, Van Krinks CH, Durham J, Tomkins SE, Burnett RD, Jones EL, Chandraratna RA, Brown G. Antagonists of retinoic acid receptors (RARs) are potent growth inhibitors of prostate carcinoma cells.Br J Cancer. 2001 Aug 3; 85(3):453-62.
| Cell experiment [1]: | |
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Cell lines |
ITS+-grown LNCaP, DU145 and PC3 cells |
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Preparation method |
The solubility of this compound in DMSO is > 16.8 mg/mL. 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. |
|
Reacting condition |
50 nM, 100 nM, 1 μM |
|
Applications |
In ITS+-grown LNCaP, DU145 and PC3 cells, AGN194310 (50 nM and 100 nM) potently inhibited colony formation. AGN194310 (1 μM) caused cells to accumulate in G1 and undergwent apoptosis. In primary prostate carcinoma cells, AGN194310 (10 and 100 nM) caused substantial growth inhibition. |
| Animal experiment [2]: | |
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Animal models |
female C57Bl/6J mice |
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Dosage form |
Oral gavage, 0.5 mg/kg/day, 11 days |
|
Application |
Treatment with AGN194310 significantly increased the number and proportion of granulocytes. Treatment with AGN194310 significantly increased the frequency of progenitor cells containing granulocytes in the bone marrow of mice. |
|
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]. Hammond L A, Van Krinks C H, Durham J, et al. Antagonists of retinoic acid receptors (RARs) are potent growth inhibitors of prostate carcinoma cells[J]. British journal of cancer, 2001, 85(3): 453. [2]. Walkley C R, Yuan Y D, Chandraratna R A S, et al. Retinoic acid receptor antagonism in vivo expands the numbers of precursor cells during granulopoiesis[J]. Leukemia, 2002, 16(9): 1763. | |
| Cas No. | 229961-45-9 | SDF | |
| Synonyms | VTP-194310 | ||
| Chemical Name | 4-((4-(4-ethylphenyl)-2,2-dimethyl-2H-thiochromen-6-yl)ethynyl)benzoic acid | ||
| Canonical SMILES | CCC1=CC=C(C(C2=C(S3)C=CC(C#CC4=CC=C(C(O)=O)C=C4)=C2)=CC3(C)C)C=C1 | ||
| Formula | C28H24O2S | M.Wt | 424.55 |
| Solubility | ≥ 16.8mg/mL in DMSO | 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 | 2.3554 mL | 11.7772 mL | 23.5544 mL |
| 5 mM | 0.4711 mL | 2.3554 mL | 4.7109 mL |
| 10 mM | 0.2355 mL | 1.1777 mL | 2.3554 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: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 1 reference(s) in Google Scholar.)
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