SR-9243
目录号 : GC13680
An LXR inverse agonist
Cas No.:1613028-81-1
Sample solution is provided at 25 µL, 10mM.
SR9243 is a liver-X-receptor (LXR) inverse agonist that induces LXR-corepressor interaction. It potently reduces cancer cell viability (IC50=15–104 nM) in MTT reduction assays in prostate (PC3 and DU-145), colorectal (SW620 and HT29), and lung (HOP-62 and NCI-H23) cancer cell lines. [1]
LXR (liver X receptor) is a member of the nuclear receptor family of transcription factors. It is an important regulator of glycolysis and lipogenesis enzyme expression.
In SW620 cells, 1 mM SR9243 treatment for 12 hours induces cell death with a robust increase in caspase 3/7 activation. In addition, SR9243 disrupts the Warburg effect, suppresses lipogenesis gene expression and lipid production in cancer cells without effecting normal cells. [1]
In colon tumor xenograft, SR9243 substantially and dose-dependently reduces tumor growth, glycolytic (GCK1, PFK2, PFK1 and LDH) and lipogenic (SCD1, FASN, and SREBP1c) enzyme expression without promoting weight loss. SR9243 also blocks tumor growth without causing immune or hepatic toxicity in vivo. [1]
Reference:
1. Flaveny CA, Griffett K, El-Gendy Bel-D et al. Broad Anti-tumor Activity of a Small Molecule that Selectively Targets the Warburg Effect and Lipogenesis. Cancer Cell. 2015 Jul 13;28(1):42-56.
| Cell experiment [1]: | |
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Cell lines |
SW620, HT-29, DU-145, PC3, NCI-H23 and HOP-62 cancer cells |
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Preparation method |
This compound is soluble in DMSO. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
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Reacting condition |
100 nM; 96 hrs |
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Applications |
In a variety of cancer cell lines, SR-9243 reduced cancer cell viability, with IC50 values ranging from 15 ~ 104 nM. In addition, SR-9243 induced apoptotic cell death and sensitized cancer cells to chemotherapeutic treatments. |
| Animal experiment [1]: | |
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Animal models |
Athymic mice bearing SW620 colon cancer xenografts |
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Dosage form |
30 or 60 mg/kg; i.p.; q.d. |
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Applications |
In athymic mice bearing SW620 colon cancer xenografts, SR-9243 substantially reduced the growth of colon cancer xenografts in a dose-dependent manner. Meanwhile, SR-9243-treated tumor-bearing mice did not show any weight loss. |
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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]. Flaveny CA, Griffett K, El-Gendy Bel-D et al. Broad Anti-tumor Activity of a Small Molecule that Selectively Targets the Warburg Effect and Lipogenesis. Cancer Cell. 2015 Jul 13;28(1):42-56. | |
| Cas No. | 1613028-81-1 | SDF | |
| Canonical SMILES | CC(C=C(C)C=C1C)=C1S(N(CC2=CC=C(C3=CC(C)=CC=C3)C=C2)CCC4=CC=CC(Br)=C4)(=O)=O.O=S=O | ||
| 分子式 | C31H32BrNO4S2 | 分子量 | 626.62 |
| 溶解度 | ≥ 25.2 mg/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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.5959 mL | 7.9793 mL | 15.9586 mL |
| 5 mM | 0.3192 mL | 1.5959 mL | 3.1917 mL |
| 10 mM | 0.1596 mL | 0.7979 mL | 1.5959 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: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet