| CAS |
No.108409-83-2 |
| 英文名称 |
FH535 |
| 别名 |
;6-Carboxyfluorescein;FH535 |
| 分子式 |
C13H10Cl2N2O4S |
| 分子量 |
361.2 |
| 溶解性 |
Soluble in DMSO(Need ultrasonic) |
| 纯度 |
≥98% |
| 外观(性状) |
Solid |
| 储存条件 |
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| MDL |
MFCD01212888 |
| SMILES |
CC1=C(C=CC(=C1)[N+](=O)[O-])NS(=O)(=O)C2=C(C=CC(=C2)Cl)Cl |
| InChIKey |
AXNUEXXEQGQWPA-UHFFFAOYSA-N |
| InChI |
InChI=1S/C13H10Cl2N2O4S/c1-8-6-10(17(18)19)3-5-12(8)16-22(20，21)13-7-9(14)2-4-11(13)15/h2-7，16H，1H3 |
| PubChem CID |
3463933 |
| 靶点 |
PPAR;Wnt/β-catenin |
| 通路 |
Cell Cycle;DNA Damage/DNA Repair;Stem Cells |
| 背景说明 |
FH535 是 Wnt/β-catenin 和 PPAR 的抑制剂，具有抗肿瘤活性。 |
| 生物活性 |
FH535 is an inhibitor of Wnt/β-catenin and PPAR， with anti-tumor activities.[1-3] |
| In Vitro |
FH535 是 Wnt/β-catenin 和 PPAR 的抑制剂。FH535 抑制 HCT116 细胞中的 PPARγ 和 PPARδ 反式激活。FH535 (15 μM) 活性取决于功能性 PPARδ，但不需要 PPAR 配体结合域中的半胱氨酸残基。FH535 抑制共激活因子 GRIP1 和 β-连环蛋白向 PPARδ 和 PPARγ 的募集。FH535 对 12 种表达 wnt/β-catenin 通路的癌细胞系有毒性作用[1]。FH535 (20 μM) 抑制胰腺癌细胞中的 β-catenin 通路，并抑制胰腺癌细胞迁移。此外，FH535 (20，40 μM) 抑制胰腺癌细胞侵袭和细胞生长[2]。FH535 抑制胰腺癌细胞中的血管生成相关基因[3]。 |
| In Vivo |
FH535 (25 mg/kg，ip) 对小鼠胰腺癌异种移植物具有抗肿瘤作用。FH535 还抑制胰腺癌异种移植物中的血管生成[2]。 |
| 细胞实验 |
Cell growth is evaluated using the MTT assay. Cells (5 × 104/well) are seeded in 24-well tissue culture plates. Blank control is treated with DMSO. After FH535 treatment， MTT is added to each well (final concentration， 0.5 mg/mL)， followed by 4-hour incubation at 37°C. The medium is removed， and 800 μL of DMSO is added to each well. The absorbance of the mixture is measured at 490 nm using a microplate enzyme-linked immunosorbent assay reader. The relative cell viability is calculated as follows: relative cell viability = (mean experimental absorbance/mean control absorbance) ×100%[2]. |
| 动物实验 |
Four-week-old female BALB/c athymic nude mice receive humane care. PANC-1 cells stably expressing firefly luciferase are injected into the left flanks of the mice in a total volume of 100 μL (0.5 × 107 cells)， and the mice are randomly assigned to a DMSO [intraperitoneally injected with 100 μL DMSO/DMEM (1:1)] or FH535 group [intraperitoneally injected with 25 mg/kg FH535 dissolved in 100 μL DMSO/DMEM (1:1)]. Treatment is conducted every 2 days for 20 days; tumor volume is measured with a caliper using the formula: volume = length × width2/2. At the end of the experiment， the mice are anaesthetized and given D-luciferin in PBS. Twenty minutes after the injection， bioluminescence is imaged with a charge-coupled device camera. Then， the tumor tissue is stripped and formalin-fixed， paraffin-embedded， cut into 4-μm sections， and immunohistochemically stained[3]. |
| 数据来源文献 |
[1]. Handeli S， et al. A small-molecule inhibitor of Tcf/beta-catenin signaling down-regulates PPARgamma and PPARdelta activities. Mol Cancer Ther. 2008 Mar;7(3):521-9.
[2]. Wu MY， et al. FH535 inhibited metastasis and growth of pancreatic cancer cells. Onco Targets Ther. 2015 Jul 6;8:1651-70.
[3]. Liu L， et al. FH535， a β-catenin pathway inhibitor， represses pancreatic cancer xenograft growth and angiogenesis. Oncotarget. 2016 Jul 26;7(30):47145-47162. |
| 规格 |
1mg 5mg 10mg 50mg 100mg |
| 单位 |
瓶 |
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