CS-1211

生物活性靶点体外研究体内研究 CS-1211 试剂级价格

CS-1211

CAS号:229961-45-9
英文名:AGN 194310
中文名:CS-1211
CBNumber:CB01346990
分子式:C28H24O2S
分子量:424.55
MOL File:229961-45-9.mol

CS-1211化学性质

沸点 :598.1±50.0 °C(Predicted)
密度 :1.26±0.1 g/cm3(Predicted)
储存条件 :Store at -20°C
溶解度 :>16.8mg/mL in DMSO
形态 :Powder
酸度系数(pKa) :4.02±0.10(Predicted)

CS-1211性质、用途与生产工艺

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)

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.

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.