| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
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| ln Vitro |
In all three cell lines, AGN194310 efficiently prevents colony formation; its IC50 values for LNCaP, PC3, and DU-145 cells are 16 nM, 18 nM, and 34 nM, respectively [2]. colony development is inhibited by AGN 194310 (50 nM, 100 nM; LNCaP, PC-3, and DU-145 cells) at 50 nM (alone) and 100 nM (with TNTPB) concentrations (2). 80% of LNCaP cells undergo apoptosis when exposed to 1 μM of AGN 194310 for 72 hours [2].
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| ln Vivo |
The number of hematopoietic interstitial granulocytes in female C57Bl/6J mice treated with AGN 194310 (0.5 mg/kg/day; oral gavage; daily; for 10 days) is increased. Following AGN194310 therapy, there was a substantial increase in the frequency of granulocyte progenitor cells in mouse bone marrow [3].
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| Cell Assay |
Cell Viability Assay[2]
Cell Types: LNCaP, PC-3 and DU-145 cells. Tested Concentrations: 50 nM, 100 nM Incubation Duration: Experimental Results: When used together with 100 nM TTNPB, there was almost complete reversal of the growth inhibitory effect of 50 nM and partial reversal of the effect of 100 nM. Apoptosis Analysis[2] Cell Types: LNCaP cells Tested Concentrations: 1 μM Incubation Duration: 72 hrs (hours) Experimental Results: Induced apoptosis in LNCaP cells. |
| Animal Protocol |
Animal/Disease Models: Female C57Bl/6J mice (Fiveweeks old (34-37 days))[3]
Doses: 0.5 mg/kg/day Route of Administration: po (oral gavage); every day; for 10 days Experimental Results: The number of granulocytes was Dramatically increased across haemopoietic compartments. Progenitor cells containing granulocytes also increased Dramatically. |
| References |
[1]. Johnson AT, et al. Synthesis and biological activity of high-affinity retinoic acid receptor antagonists. Bioorg Med Chem. 1999 Jul;7(7):1321-38.
[2]. Hammond LA, et al. Antagonists of retinoic acid receptors (RARs) are potent growth inhibitors of prostate carcinoma cells. Br J Cancer. 2001 Aug 3;85(3):453-62. [3]. Walkley CR, et al. Retinoic acid receptor antagonism in vivo expands the numbers of precursor cells during granulopoiesis. Leukemia. 2002 Sep;16(9):1763-72. |
| Molecular Formula |
C28H24O2S
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|---|---|
| Molecular Weight |
424.55
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| CAS # |
229961-45-9
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| SMILES |
CC(S1)(C)C=C(C2=CC=C(CC)C=C2)C3=C1C=CC(C#CC4=CC=C(C(O)=O)C=C4)=C3
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| Solubility (In Vitro) |
DMSO : 50 mg/mL (117.77 mM)
H2O : 1 mg/mL (2.36 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1 mg/mL (2.36 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1 mg/mL (2.36 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*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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