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Purity: ≥98%
FH535 (FH-535; FH 535) is a novel and potent dual inhibitor of the Wnt/β-catenin and the PPAR (γ/δ) pathways with potential antitumor activity. It shows potent anti-proliferative activity in vitro against various cancer cells such as colon, lung, and hepatocellular carcinomas but not normal fibroblasts. FH535 also exhibits excellent in vivo antitumor efficacy in pancreatic cancer xenografts.
| ln Vitro |
FH535 inhibits both PPAR and Wnt/β-catenin. In HCT116 cells, FH535 prevents PPARγ and PPARδ transactivation. FH535 (15 μM) action does not require cysteine residues in the PPAR ligand-binding domain, but it does depend on functional PPARδ. The coactivators GRIP1 and β-catenin are not able to bind to PPARδ and PPARγ when FH535 is present. Twelve cancer cell lines that exhibit the wnt/β-catenin pathway are toxically affected by FH535 [1]. FH535 (20 μM) suppresses the migration of pancreatic cancer cells and the β-catenin pathway in these cells. Furthermore, FH535 (20, 40 μM) suppresses the proliferation and invasion of pancreatic cancer cells [2]. In pancreatic cancer cells, FH535 suppresses genes linked to angiogenesis [3].
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| ln Vivo |
On mouse pancreatic cancer xenografts, FH535 (25 mg/kg, ip) exhibits anticancer activity. Additionally, FH535 prevents angiogenesis in xenografts of pancreatic cancer [2].
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| References |
[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 |
| Molecular Formula |
C13H10CL2N2O4S
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| Molecular Weight |
361.20
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| CAS # |
108409-83-2
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| Related CAS # |
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| SMILES |
O=S(C1=CC(Cl)=CC=C1Cl)(NC2=CC=C([N+]([O-])=O)C=C2C)=O
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| InChi Key |
AXNUEXXEQGQWPA-UHFFFAOYSA-N
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| InChi Code |
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
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| Chemical Name |
2,5-dichloro-N-(2-methyl-4-nitrophenyl)-benzenesulfonamide
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| Synonyms |
FH-535; FH535; FH 535;
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7685 mL | 13.8427 mL | 27.6855 mL | |
| 5 mM | 0.5537 mL | 2.7685 mL | 5.5371 mL | |
| 10 mM | 0.2769 mL | 1.3843 mL | 2.7685 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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FH535 inhibited pancreatic cancer cell migration.Onco Targets Ther.2015 Jul 6;8:1651-70. |
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FH535 inhibited pancreatic cancer cell invasion.Onco Targets Ther.2015 Jul 6;8:1651-70. |
Inhibitory effect of FH535 on pancreatic cancer cell growth.Onco Targets Ther.2015 Jul 6;8:1651-70. |
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