产品描述
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].
体外活性
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].
体内活性
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].
Cas No.
229961-45-9
分子式
C28H24O2S
分子量
424.55
别名
VTP-194310
储存和溶解度
DMSO:50 mg/mL (117.77 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years