CS-1211
中文名称:
CS-1211
中文同义词:
RAR激动剂(AGN194310)
英文名称:
AGN 194310
英文同义词:
AGN 194310;AGN-194310, 194310;CS-1211;AGN194310; AGN-194310; VTP194310; VTP 194310; VTP-194310;VTP 194310;VTP194310;VTP-194310;AGN
CAS号:
229961-45-9
分子式:
C28H24O2S
分子量:
424.55
EINECS号:
相关类别:
细胞生物学试剂
Mol文件:
229961-45-9.mol
生物活性
AGN 194310 (VTP-194310) 是一种高亲和力的、有效的、具有选择性的视黄酸受体 (RARs) 的泛拮抗剂，对 RARα，RARβ，RARγ 的 Kd 值分别为 3 nM，2 nM，5 nM。
靶点
RARα
3 nM (Kd)
RARβ
2 nM (Kd)
RARγ
5 nM (Kd)
RARα
3 nM (Kd)
RARβ
2 nM (Kd)
体外研究
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.
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.
AGN 194310 (1 μM; 72 hours; LNCaP cells) treatment results in 80% apoptosis.
Cell Viability Assay
Cell 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 Analysis
Cell Line: LNCaP cells
Concentration: 1 μM
Incubation Time: 72 hours
Result: Induced apoptosis in LNCaP cells.
Cell 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.
Cell Line:
LNCaP cells
Concentration:
1 μM
Incubation Time:
72 hours
Result:
Induced apoptosis in LNCaP cells.
体内研究
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.
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.
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.
