AGN 194310 (C007B-325197)

AGN 194310 (VTP-194310) is a high affinity, potent and selective retinioic acid receptors (RARs) pan-antagonist with K d values of 3 nM, 2 nM, 5 nM for RARα , RARβ , RARγ , respectively.In VitroAGN194310 potently inhibits colony formation by all three lines, with IC 50 values of 16 nM for LNCaP cells; 18 nM for PC3 cells; and 34 nM for DU-145 cells. ?/nAGN 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. ?/nAGN 194310 (1 μM; 72 hours; LNCaP cells) treatment results in 80% apoptosis. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: LNCaP, PC-3 and DU-145 cells. Concentration: 50 nM, 100 nM Incubation Time: Result: 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 AnalysisCell Line: LNCaP cells Concentration: 1 μM Incubation Time: 72 hours Result: Induced apoptosis in LNCaP cells.In VivoAGN 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female C57Bl/6J mice (Five-week-old (34-37 days))Dosage: 0.5 mg/kg/day Administration: Oral gavage; every day; for 10 days Result: The number of granulocytes was significantly increased across haemopoietic compartments. Progenitor cells containing granulocytes also increased significantly.Form:Solid. Specification: 0.98 Molecular Formula: C28H24O2S Molecular Weight: 424.55 PubChem CID: 9867046 Isomeric SMILES: CCC1=CC=C(C=C1)C2=CC(SC3=C2C=C(C=C3)C#CC4=CC=C(C=C4)C(=O)O)(C)C