FH535 |
| رقم الكتالوجGC12134 |
An inhibitor of β-catenin signaling
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 108409-83-2
Sample solution is provided at 25 µL, 10mM.
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FH535 is a small molecule inhibitor of Wnt/B-catenin with IC50 values of 15.4μM, 10.9μM, 9.3μM, respectively in LCSC, Huh7, PLC cell lines [1].
FH535 can inhibit the growth of colon, lung, and hepatocellular carcinoma line but not normal fibroblasts. It makes FH535 potentially be a promising therapeutic approach for cancer cells. It is reported that FH535 has ability to inhibit growth, migration, and invasion of TN breast cancer cell lines (MDA-MB-231 and HCC38) without affecting adhesive abilities of cells to type I collagen [2].
FH535 is also an inhibitor of peroxisome proliferator–activated receptor (PPAR). It plays a role as a dual PPARγ and PPARδ antagonist that is able to inhibit GRIP1 and β-catenin recruitment [3].
References:
[1] Roberto R. Galuppo, Roberto Gedaly, Paul Angulo, Michael F. et al. FH535 inhibits wnt/β-catenin signaling pathway in liver cancer stem cells and HCC cell lines. Hepatology. 2013, October: 466A.
[2] Joji Iida, Jesse Dorchak, John R. Lehman, Rebecca Clancy, Chunqing Luo, Yaqin Chen, Stella Somiari, Rachel E. Ellsworth, Hai Hu, Richard J. Mural, Craig D. Shriver. FH535 Inhibited Migration and Growth of Breast Cancer
Cells. PLOS ONE. 2012, 7(9): 1-11.
[3] Shlomo Handeli and Julian A. Simon. A small-molecule inhibitor of Tcf/β-catenin signaling down-regulates PPARγ and PPARδ activities. Molecular Cancer Therapeutics. 2008, 7:521-529.
| Kinase experiment [1]: | |
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High-throughput library screen |
Three copies of the optimized or mutated Tcf-binding element from TOPFLASH or FOPFLASH driving a secreted alkaline phosphatase reporter gene were cloned into pCEP4 plasmid, replacing the cytomegalovirus promoter. The plasmids were transfected into HepG2 cells, and Hygromycin-resistant clones were pooled. Library screening was done at 20 μmol/L concentration in HepG2 serum-free media. Hits were tested in the HCT116 cell line for inhibition of TOPFLASH luciferase activity but not for inhibition of a reporter activity controlled from β-actin promoter. |
| Cell experiment [1]: | |
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Cell lines |
HCT116, SW48, RKO, LoVo, COLO205, IEC6, A427, HCC15, NCI-H1703, A549, HepG2, Hep3b, Huh7 and fibroblasts |
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Preparation method |
The solubility of this compound in DMSO is >10 mM. 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. |
|
Reaction Conditions |
30 μM; 48 hrs |
|
Applications |
FH535 showed selective anti-proliferation effect on some cancer cells (HCT116, SW48, RKO, LoVo, COLO205, A427, HCC15, NCI-H1703, A549, HepG2, Hep3b and Huh7 cells) expressing high or active Wnt/β-catenin pathway. |
| Animal experiment [2]: | |
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Animal models |
Nude mouse bearing pancreatic cancer xenografts |
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Dosage form |
25 mg/kg; i.p.; every 2 days for 20 days |
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Applications |
FH535 significantly repressed pancreatic cancer xenograft growth in vivo and showed better performance status with respect to body weight loss. |
|
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]. Shlomo Handeli and Julian A. Simon. A small-molecule inhibitor of Tcf/β-catenin signaling down-regulates PPARγ and PPARδ activities. Molecular Cancer Therapeutics. 2008, 7:521-529. [2]. Liu L, Zhi Q, Shen M, Gong FR, Zhou BP, Lian L, Shen B, Chen K, Duan W, Wu MY, Tao M, Li W. FH535, a β-catenin pathway inhibitor, represses pancreatic cancer xenograft growth and angiogenesis. Oncotarget. 2016 Jun 13. | |
| Cas No. | 108409-83-2 | SDF | |
| Chemical Name | 2,5-dichloro-N-(2-methyl-4-nitrophenyl)benzenesulfonamide | ||
| Canonical SMILES | CC1=C(C=CC(=C1)[N+](=O)[O-])NS(=O)(=O)C2=C(C=CC(=C2)Cl)Cl | ||
| Formula | C13H10Cl2N2O4S | M.Wt | 361.2 |
| الذوبان | ≥ 36.1 mg/mL in DMSO, ≥ 5.87 mg/mL in EtOH with gentle warming | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.7685 mL | 13.8427 mL | 27.6855 mL |
| 5 mM | 553.7 μL | 2.7685 mL | 5.5371 mL |
| 10 mM | 276.9 μL | 1.3843 mL | 2.7685 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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