FH535
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MedKoo CAT#: 407354

CAS#: 108409-83-2

Description: FH535 is a β-catenin pathway inhibitor. FH535 represses pancreatic cancer xenograft growth and angiogenesis. FH535 increases the radiosensitivity and reverses epithelial-to-mesenchymal transition of radioresistant esophageal cancer cell line KYSE-150R. FH535 inhibited metastasis and growth of pancreatic cancer cells. FH535 selectively inhibits cell proliferation and potentiates imatinib-induced apoptosis in myeloid leukemia cell lines.

Chemical Structure

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FH535
CAS# 108409-83-2
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 407354
Name: FH535
CAS#: 108409-83-2
Chemical Formula: C13H10Cl2N2O4S
Exact Mass: 359.97
Molecular Weight: 361.193
Elemental Analysis: C, 43.23; H, 2.79; Cl, 19.63; N, 7.76; O, 17.72; S, 8.88

Price and Availability

Size Price Availability Quantity
100mg USD 650
200mg USD 1050
500mg USD 1950
1g USD 2850
2g USD 3950
5g USD 5450
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Synonym: FH535; FH 535; FH-535.

IUPAC/Chemical Name: 2,5-dichloro-N-(2-methyl-4-nitrophenyl)-benzenesulfonamide

InChi Key: AXNUEXXEQGQWPA-UHFFFAOYSA-N

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

SMILES Code: O=S(C1=CC(Cl)=CC=C1Cl)(NC2=CC=C([N+]([O-])=O)C=C2C)=O

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Product Data:
Product Data
Instruction:
View handling instruction
Biological target: FH535 is an inhibitor of Wnt/β-catenin and PPAR, with anti-tumor activities.
In vitro activity: FH535 could significantly suppress the growth of DLD-1 and SW620 cells in a concentration-dependent and time-dependent manner. The results of cell cycle tests showed that FH535 could significantly induce G2/M arrest in colorectal cancer cells. Reference: Gene. 2019 Mar 30;690:48-56. https://pubmed.ncbi.nlm.nih.gov/30552982/
In vivo activity: To investigate whether FH535 has inhibitory effect on colon cancer growth in vivo, this study evaluated the effect of this chemical on HT29 nude mice xenografts. 12 days after the initiation of FH535 treatment, the calculated tumor volume of the FH535-treated group reached statistical significance as compared to the control group (Figure 2A). At the end of the experiment, the tumor size and weight of FH535-treated group was significantly smaller than the control group (Figure 2B-C). Reference: J Cancer. 2017; 8(16): 3142–3153. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5665030/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 35.6 98.59
DMF 25.0 69.22
DMF:PBS (pH 7.2) (1:1) 0.5 1.38

Preparing Stock Solutions

The following data is based on the product molecular weight 361.19 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Tu X, Hong D, Jiang Y, Lou Z, Wang K, Jiang Y, Jin L. FH535 inhibits proliferation and migration of colorectal cancer cells by regulating CyclinA2 and Claudin1 gene expression. Gene. 2019 Mar 30;690:48-56. doi: 10.1016/j.gene.2018.12.008. Epub 2018 Dec 12. PMID: 30552982. 2. Shi M, Cheng J, He Y, Jiang Z, Bodinga BM, Liu B, Chen H, Li Q. Effect of FH535 on in vitro maturation of porcine oocytes by inhibiting WNT signaling pathway. Anim Sci J. 2018 Apr;89(4):631-639. doi: 10.1111/asj.12982. Epub 2017 Dec 28. PMID: 29284185. 3. Chen Y, Rao X, Huang K, Jiang X, Wang H, Teng L. FH535 Inhibits Proliferation and Motility of Colon Cancer Cells by Targeting Wnt/β-catenin Signaling Pathway. J Cancer. 2017 Sep 12;8(16):3142-3153. doi: 10.7150/jca.19273. PMID: 29158786; PMCID: PMC5665030. 4. 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 Jul 26;7(30):47145-47162. doi: 10.18632/oncotarget.9975. PMID: 27323403; PMCID: PMC5216931.
In vitro protocol: 1. Tu X, Hong D, Jiang Y, Lou Z, Wang K, Jiang Y, Jin L. FH535 inhibits proliferation and migration of colorectal cancer cells by regulating CyclinA2 and Claudin1 gene expression. Gene. 2019 Mar 30;690:48-56. doi: 10.1016/j.gene.2018.12.008. Epub 2018 Dec 12. PMID: 30552982. 2. Shi M, Cheng J, He Y, Jiang Z, Bodinga BM, Liu B, Chen H, Li Q. Effect of FH535 on in vitro maturation of porcine oocytes by inhibiting WNT signaling pathway. Anim Sci J. 2018 Apr;89(4):631-639. doi: 10.1111/asj.12982. Epub 2017 Dec 28. PMID: 29284185.
In vivo protocol: 1. Chen Y, Rao X, Huang K, Jiang X, Wang H, Teng L. FH535 Inhibits Proliferation and Motility of Colon Cancer Cells by Targeting Wnt/β-catenin Signaling Pathway. J Cancer. 2017 Sep 12;8(16):3142-3153. doi: 10.7150/jca.19273. PMID: 29158786; PMCID: PMC5665030. 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 Jul 26;7(30):47145-47162. doi: 10.18632/oncotarget.9975. PMID: 27323403; PMCID: PMC5216931.

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1: 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 Jul 26;7(30):47145-47162. doi: 10.18632/oncotarget.9975. PubMed PMID: 27323403.

2: Su H, Jin X, Zhang X, Zhao L, Lin B, Li L, Fei Z, Shen L, Fang Y, Pan H, Xie C. FH535 increases the radiosensitivity and reverses epithelial-to-mesenchymal transition of radioresistant esophageal cancer cell line KYSE-150R. J Transl Med. 2015 Mar 31;13:104. doi: 10.1186/s12967-015-0464-6. PubMed PMID: 25888911; PubMed Central PMCID: PMC4384308.

3: Wu MY, Liang RR, Chen K, Shen M, Tian YL, Li DM, Duan WM, Gui Q, Gong FR, Lian L, Li W, Tao M. FH535 inhibited metastasis and growth of pancreatic cancer cells. Onco Targets Ther. 2015 Jul 6;8:1651-70. doi: 10.2147/OTT.S82718. PubMed PMID: 26185454; PubMed Central PMCID: PMC4500609.

4: Suknuntha K, Thita T, Togarrati PP, Ratanachamnong P, Wongtrakoongate P, Srihirun S, Slukvin I, Hongeng S. Wnt signaling inhibitor FH535 selectively inhibits cell proliferation and potentiates imatinib-induced apoptosis in myeloid leukemia cell lines. Int J Hematol. 2016 Oct 20. [Epub ahead of print] PubMed PMID: 27766528.

5: Tomizawa M, Shinozaki F, Motoyoshi Y, Sugiyama T, Yamamoto S, Ishige N. FH535 suppresses the proliferation and motility of hepatocellular carcinoma cells. Int J Oncol. 2016 Jan;48(1):110-4. doi: 10.3892/ijo.2015.3220. PubMed PMID: 26530115.

6: Gedaly R, Galuppo R, Daily MF, Shah M, Maynard E, Chen C, Zhang X, Esser KA, Cohen DA, Evers BM, Jiang J, Spear BT. Targeting the Wnt/β-catenin signaling pathway in liver cancer stem cells and hepatocellular carcinoma cell lines with FH535. PLoS One. 2014 Jun 18;9(6):e99272. doi: 10.1371/journal.pone.0099272. PubMed PMID: 24940873; PubMed Central PMCID: PMC4062395.

7: Liu J, Li G, Liu D, Liu J. FH535 inhibits the proliferation of HepG2 cells via downregulation of the Wnt/β-catenin signaling pathway. Mol Med Rep. 2014 Apr;9(4):1289-92. doi: 10.3892/mmr.2014.1928. PubMed PMID: 24482011.

8: Iida J, Dorchak J, Lehman JR, Clancy R, Luo C, Chen Y, Somiari S, Ellsworth RE, Hu H, Mural RJ, Shriver CD. FH535 inhibited migration and growth of breast cancer cells. PLoS One. 2012;7(9):e44418. doi: 10.1371/journal.pone.0044418. PubMed PMID: 22984505; PubMed Central PMCID: PMC3439405.

9: Polk WW. FH535 potentiation of cigarette smoke condensate cytotoxicity is associated with changes in β-catenin and EGR-1 signaling. Int J Toxicol. 2012 Jul-Aug;31(4):380-9. doi: 10.1177/1091581812447956. PubMed PMID: 22713211.

10: Kril LM, Vilchez V, Jiang J, Turcios L, Chen C, Sviripa VM, Zhang W, Liu C, Spear B, Watt DS, Gedaly R. N-Aryl benzenesulfonamide inhibitors of [3H]-thymidine incorporation and β-catenin signaling in human hepatocyte-derived Huh-7 carcinoma cells. Bioorg Med Chem Lett. 2015 Sep 15;25(18):3897-9. doi: 10.1016/j.bmcl.2015.07.040. PubMed PMID: 26243371; PubMed Central PMCID: PMC4540627.

11: Galuppo R, Maynard E, Shah M, Daily MF, Chen C, Spear BT, Gedaly R. Synergistic inhibition of HCC and liver cancer stem cell proliferation by targeting RAS/RAF/MAPK and WNT/β-catenin pathways. Anticancer Res. 2014 Apr;34(4):1709-13. PubMed PMID: 24692700.

12: Umazume K, Tsukahara R, Liu L, Fernandez de Castro JP, McDonald K, Kaplan HJ, Tamiya S. Role of retinal pigment epithelial cell β-catenin signaling in experimental proliferative vitreoretinopathy. Am J Pathol. 2014 May;184(5):1419-28. doi: 10.1016/j.ajpath.2014.01.022. PubMed PMID: 24656918.

13: Handeli S, Simon JA. A small-molecule inhibitor of Tcf/beta-catenin signaling down-regulates PPARgamma and PPARdelta activities. Mol Cancer Ther. 2008 Mar;7(3):521-9. doi: 10.1158/1535-7163.MCT-07-2063. PubMed PMID: 18347139.

14: Wu MY, Xie X, Xu ZK, Xie L, Chen Z, Shou LM, Gong FR, Xie YF, Li W, Tao M. PP2A inhibitors suppress migration and growth of PANC-1 pancreatic cancer cells through inhibition on the Wnt/β-catenin pathway by phosphorylation and degradation of β-catenin. Oncol Rep. 2014 Aug;32(2):513-22. doi: 10.3892/or.2014.3266. PubMed PMID: 24926961; PubMed Central PMCID: PMC4091883.

15: Wachter J, Neureiter D, Alinger B, Pichler M, Fuereder J, Oberdanner C, Di Fazio P, Ocker M, Berr F, Kiesslich T. Influence of five potential anticancer drugs on wnt pathway and cell survival in human biliary tract cancer cells. Int J Biol Sci. 2012;8(1):15-29. PubMed PMID: 22211101; PubMed Central PMCID: PMC3226029.

16: Iwata M, Aikawa T, Hakozaki T, Arai K, Ochi H, Haro H, Tagawa M, Asou Y, Hara Y. Enhancement of Runx2 expression is potentially linked to β-catenin accumulation in canine intervertebral disc degeneration. J Cell Physiol. 2015 Jan;230(1):180-90. doi: 10.1002/jcp.24697. PubMed PMID: 24916026.

17: Kim HJ, Kang GJ, Kim EJ, Park MK, Byun HJ, Nam S, Lee H, Lee CH. Novel effects of sphingosylphosphorylcholine on invasion of breast cancer: Involvement of matrix metalloproteinase-3 secretion leading to WNT activation. Biochim Biophys Acta. 2016 Sep;1862(9):1533-43. doi: 10.1016/j.bbadis.2016.05.010. PubMed PMID: 27216977.

18: Ren J, Wang R, Song H, Huang G, Chen L. Secreted frizzled related protein 1 modulates taxane resistance of human lung adenocarcinoma. Mol Med. 2014 Apr 8;20:164-78. doi: 10.2119/molmed.2013.00149. PubMed PMID: 24643460; PubMed Central PMCID: PMC4002848.

19: Zhang S, Da L, Yang X, Feng D, Yin R, Li M, Zhang Z, Jiang F, Xu L. Celecoxib potentially inhibits metastasis of lung cancer promoted by surgery in mice, via suppression of the PGE2-modulated β-catenin pathway. Toxicol Lett. 2014 Mar 3;225(2):201-7. doi: 10.1016/j.toxlet.2013.12.014. PubMed PMID: 24374173.

20: Frewer KA, Sanders AJ, Owen S, Frewer NC, Hargest R, Jiang WG. A role for WISP2 in colorectal cancer cell invasion and motility. Cancer Genomics Proteomics. 2013 Jul-Aug;10(4):187-96. PubMed PMID: 23893926.