GlpBio

AGN 194310

目录号: GC12598纯度: >98.00%同义词: VTP-194310
AGN 194310 (VTP-194310) 是一种高亲和力、有效和选择性的视黄酸受体 (RARs) 泛拮抗剂，对 RARα、RARβ、RARγ 的 Kd 值分别为 3 nM、2 nM、5 nM。
AGN 194310
Cas No.: 229961-45-9
规格价格库存数量操作
1mg¥1,080.00现货
1
5mg¥4,050.00现货
1
10mM (in 1mL DMSO)¥4,455.00现货
1
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产品描述 Description

AGN 194310 is a pan-antagonist of retinoic acid receptors (RARs) with Kd values of 3nM, 2nM and 5nM for RAR α, RARβ and RARγ, respectively [1].

AGN 194310 has been reported to bind to RARs with equal and high Kd values of 3, 2 and 5nM for RAR α, RARβ and RARγ, respectively, by in vitro binding experiments. In addition, AGN 194310 has been revealed to potently inhibit the colony formation by ITS+-grown cell lines with IC50 values of 16 ± 5nM for LNCaP cells; 18 ± 6nM for PC3 cells; and 34 ± 7nM for DU-145 cells. Apart from these, because of binding to and mediating the effects via RARs, AGN 194310 has been demonstrated to inhibit agonist-induced (TTNPB) differentiation of HL60 cells. AGN 194310 has also shown the accumulation of cell in G1 and the function of induced apoptosis [1].

References:
[1] Hammond LA1, Van Krinks CH, Durham J, Tomkins SE, Burnett RD, Jones EL, Chandraratna RA, Brown G. Antagonists of retinoic acid receptors (RARs) are potent growth inhibitors of prostate carcinoma cells.Br J Cancer. 2001 Aug 3; 85(3):453-62.

实验参考方法 Experimental Reference Method

Cell experiment [1]:

Cell lines

ITS+-grown LNCaP, DU145 and PC3 cells

Preparation method

The solubility of this compound in DMSO is > 16.8 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

50 nM, 100 nM, 1 μM

Applications

In ITS+-grown LNCaP, DU145 and PC3 cells, AGN194310 (50 nM and 100 nM) potently inhibited colony formation. AGN194310 (1 μM) caused cells to accumulate in G1 and undergwent apoptosis. In primary prostate carcinoma cells, AGN194310 (10 and 100 nM) caused substantial growth inhibition.
Animal experiment [2]:

Animal models

female C57Bl/6J mice

Dosage form

Oral gavage, 0.5 mg/kg/day, 11 days

Application

Treatment with AGN194310 significantly increased the number and proportion of granulocytes. Treatment with AGN194310 significantly increased the frequency of progenitor cells containing granulocytes in the bone marrow of mice.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Hammond L A, Van Krinks C H, Durham J, et al. Antagonists of retinoic acid receptors (RARs) are potent growth inhibitors of prostate carcinoma cells[J]. British journal of cancer, 2001, 85(3): 453.

[2]. Walkley C R, Yuan Y D, Chandraratna R A S, et al. Retinoic acid receptor antagonism in vivo expands the numbers of precursor cells during granulopoiesis[J]. Leukemia, 2002, 16(9): 1763.

产品文档 Product Documents

Purity:>98.00%

化学性质Chemical Properties

CAS 号
229961-45-9
同义词
VTP-194310
化学名
4-((4-(4-ethylphenyl)-2,2-dimethyl-2H-thiochromen-6-yl)ethynyl)benzoic acid
SMILES
CCC1=CC=C(C(C2=C(S3)C=CC(C#CC4=CC=C(C(O)=O)C=C4)=C2)=CC3(C)C)C=C1
分子式
C28H24O2S
分子量
424.55 g/mol
溶解性
≥ 16.8mg/mL in DMSO
保存条件
Store at -20°C
General tips
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol