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AGN 194310

Catalog No. T14143   CAS 229961-45-9
Synonyms: VTP-194310

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].

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AGN 194310 Chemical Structure
AGN 194310, CAS 229961-45-9
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5 mg 8-10 weeks $ 596.00
25 mg 8-10 weeks $ 1,710.00
50 mg 8-10 weeks $ 2,230.00
100 mg 8-10 weeks $ 3,390.00
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Biological Description
Chemical Properties
Storage & Solubility Information
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].
Targets&IC50 RARβ:2 nM (kd), RARγ:5 nM (kd), RARα:3 nM (kd)
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].
Synonyms VTP-194310
Molecular Weight 424.55
Formula C28H24O2S
CAS No. 229961-45-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (117.77 mM), Sonification is recommended.

TargetMolReferences and Literature

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.

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Keywords

AGN 194310 229961-45-9 Metabolism Retinoid Receptor VTP-194310 AGN-194310 AGN194310 VTP 194310 VTP194310 inhibitor inhibit

 

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