AGN 194310(Synonyms: VTP-194310)

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AGN 194310 (Synonyms: VTP-194310) 纯度: 98.01%

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。

AGN 194310(Synonyms: VTP-194310)

AGN 194310 Chemical Structure

CAS No. : 229961-45-9

规格 价格 是否有货 数量
1 mg ￥1500 In-stock
5 mg ￥5500 In-stock
10 mg ￥8500 In-stock
25 mg ￥14500 In-stock
50 mg ￥22500 In-stock
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200 mg   询价  

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生物活性

AGN 194310 (VTP-194310) is a high affinity, potent and selective retinioic acid receptors (RARs) pan-antagonist with Kd values of 3 nM, 2 nM, 5 nM for RARα, RARβ, RARγ, respectively[1][2].

IC50 & Target[1]

RARα

3 nM (Kd)

RARβ

2 nM (Kd)

RARγ

5 nM (Kd)

体外研究
(In Vitro)

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[2]

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[2]

Cell Line: LNCaP cells
Concentration: 1 μM
Incubation Time: 72 hours
Result: Induced apoptosis in LNCaP cells.

体内研究
(In Vivo)

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female C57Bl/6J mice (Five-week-old (34-37 days))[3]
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.

分子量

424.55

Formula

C28H24O2S
CAS 号

229961-45-9
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 50 mg/mL (117.77 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.3554 mL 11.7772 mL 23.5544 mL
5 mM 0.4711 mL 2.3554 mL 4.7109 mL
10 mM 0.2355 mL 1.1777 mL 2.3554 mL

*

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, 6 months; -20°C, 1 month。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.89 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.89 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.89 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.89 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Johnson AT, et al. Synthesis and biological activity of high-affinity retinoic acid receptor antagonists. Bioorg Med Chem. 1999 Jul;7(7):1321-38.

    [2]. Hammond LA, et al. Antagonists of retinoic acid receptors (RARs) are potent growth inhibitors of prostate carcinoma cells. Br J Cancer. 2001 Aug 3;85(3):453-62.

    [3]. Walkley CR, et al. Retinoic acid receptor antagonism in vivo expands the numbers of precursor cells during granulopoiesis. Leukemia. 2002 Sep;16(9):1763-72.

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