AGN 194310
(Synonyms: VTP-194310) 目录号 : GC12598
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。
Cas No.:229961-45-9
Sample solution is provided at 25 µL, 10mM.
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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.
| Cell experiment [1]: | |
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Cell lines |
ITS+-grown LNCaP, DU145 and PC3 cells |
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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. |
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Reacting condition |
50 nM, 100 nM, 1 μM |
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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]: | |
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Animal models |
female C57Bl/6J mice |
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Dosage form |
Oral gavage, 0.5 mg/kg/day, 11 days |
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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. |
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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. |
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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. |
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| Cas No. | 229961-45-9 | SDF | |
| 别名 | VTP-194310 | ||
| 化学名 | 4-((4-(4-ethylphenyl)-2,2-dimethyl-2H-thiochromen-6-yl)ethynyl)benzoic acid | ||
| Canonical 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 |
| 溶解度 | ≥ 16.8mg/mL in DMSO | 储存条件 | 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℃，然后在超声波浴中震荡一段时间。 |
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| 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。 | ||
| 制备储备液 | |||
 |
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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet