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229961-45-9

中文名稱 CS-1211
英文名稱 AGN 194310
CAS 229961-45-9
分子式 C28H24O2S
分子量 424.55
MOL 文件 229961-45-9.mol
更新日期 2024/11/15 18:20:34
229961-45-9 結(jié)構(gòu)式 229961-45-9 結(jié)構(gòu)式

基本信息

中文別名
RAR激動(dòng)劑(AGN194310)
英文別名
AGN
CS-1211
VTP194310
VTP-194310
AGN 194310
VTP 194310
AGN-194310, 194310
AGN194310
AGN-194310
VTP194310
VTP 194310
VTP-194310
Benzoic acid, 4-[2-[4-(4-ethylphenyl)-2,2-dimethyl-2H-1-benzothiopyran-6-yl]ethynyl]-
所屬類別
生物化工:激動(dòng)劑抑制劑

物理化學(xué)性質(zhì)

沸點(diǎn)598.1±50.0 °C(Predicted)
密度1.26±0.1 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度>16.8mg/mL in DMSO
酸度系數(shù)(pKa)4.02±0.10(Predicted)
形態(tài)粉末
顏色White to off-white

常見問題列表

生物活性
AGN 194310 (VTP-194310) 是一種高親和力的、有效的、具有選擇性的視黃酸受體 (RARs) 的泛拮抗劑,對(duì) RARα,RARβ,RARγ 的 Kd 值分別為 3 nM,2 nM,5 nM。
靶點(diǎn)

RARα

3 nM (Kd)

RARβ

2 nM (Kd)

RARγ

5 nM (Kd)

體外研究

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.
體內(nèi)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.
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