| Description | AGN 194310 (VTP-194310) is retinioic acid receptors (RARs) pan-antagonist. The Kd values of 3 nM, 2 nM, 5 nM for RARα, RARβ, RARγ, respectively[1][2]. |
| In vitro | AGN194310 potently inhibits colony formation by all three lines, with IC50 values of 16 nM for LNCaP cells; 18 nM for PC3 cells; and 34 nM for DU-145 cells[2]. AGN 194310 (50 nM, 100 nM; LNCaP, PC-3 and DU-145 cells) inhibits colony formation at concentrations of 50 nM and 100 nM alone and in combination with TTNPB[2]. AGN 194310 (1 μM; 72 hours; LNCaP cells) treatment results in 80% apoptosis[2]. |
| In vivo | AGN 194310 (0.5 mg/kg/day; oral gavage; every day; for 10 days; female C57Bl/6J mice) treatment increases the number of granulocytes across haemopoietic compartments. A significant increase in the frequency of granulocyte-progenitor cells is observed in the bone marrow of mice after treatment with AGN194310[3]. |
| Target activity | RARβ:2 nM （kd）, RARγ:5 nM （kd）, RARα:3 nM （kd） |
| Synonyms | VTP-194310 |
| molecular weight | 424.55 |
| Molecular formula | C28H24O2S |
| CAS | 229961-45-9 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 50 mg/mL (117.77 mM), Sonication is recommended. |
| 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. |