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CWP232228

  Cat. No.:  DC29001   Featured
Chemical Structure
1144044-02-9
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More than 5000 active chemicals with high quality for research!
Field of application
CWP232228, a highly potent selective Wnt/β-catenin signaling inhibitor, antagonizes binding of β-catenin to T-cell factor (TCF) in the nucleus. CWP232228 suppresses tumor formation and metastasis without toxicity through the inhibition of the growth of breast and liver cancer stem cells (CSCs).
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1144044-02-9
Chemical Name: CWP232228
Synonyms: CWP232228 sodium;Sodium 4-(((6S,9aS)-2-Allyl-1-(benzylcarbamoyl)-8-((2-methyl-2H-indazol-7-yl)methyl)-4,7-dioxooctahydro-2H-pyrazino[2,1-c][1,2,4]triazin-6-yl)methyl)phenyl phosphate;Sodium 4-(((6S,9aS)-2-allyl-1-(benzylcarbamoyl)-8-((2-methyl-2H-indazol-7-yl)methyl)-4,7-dioxooctahydro-1H-pyrazino[2,1-c][1,2,4]triazin-6-yl)methyl)phenyl phosphate;CWP232228
SMILES: P(=O)([O-])([O-])OC1C=CC(=CC=1)C[C@H]1C(N(CC2=CC=CC3=CN(C)N=C23)C[C@@H]2N(C(NCC3C=CC=CC=3)=O)N(CC=C)CC(N21)=O)=O.[Na+].[Na+]
Formula: C33H34N7Na2O7P
M.Wt: 717.619069576263
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication: 1: Jang GB, Hong IS, Kim RJ, Lee SY, Park SJ, Lee ES, Park JH, Yun CH, Chung JU, Lee KJ, Lee HY, Nam JS. Wnt/β-Catenin Small-Molecule Inhibitor CWP232228 Preferentially Inhibits the Growth of Breast Cancer Stem-like Cells. Cancer Res. 2015 Apr 15;75(8):1691-702. doi: 10.1158/0008-5472.CAN-14-2041. Epub 2015 Feb 6. PubMed PMID: 25660951. 2: Kim JY, Lee HY, Park KK, Choi YK, Nam JS, Hong IS. CWP232228 targets liver cancer stem cells through Wnt/β-catenin signaling: a novel therapeutic approach for liver cancer treatment. Oncotarget. 2016 Apr 12;7(15):20395-409. doi: 10.18632/oncotarget.7954. PubMed PMID: 26967248; PubMed Central PMCID: PMC4991463. 3: Benoit YD, Mitchell RR, Risueño RM, Orlando L, Tanasijevic B, Boyd AL, Aslostovar L, Salci KR, Shapovalova Z, Russell J, Eguchi M, Golubeva D, Graham M, Xenocostas A, Trus MR, Foley R, Leber B, Collins TJ, Bhatia M. Sam68 Allows Selective Targeting of Human Cancer Stem Cells. Cell Chem Biol. 2017 Jul 20;24(7):833-844.e9. doi: 10.1016/j.chembiol.2017.05.026. Epub 2017 Jun 22. PubMed PMID: 28648376. 4: Katoh M. Canonical and non-canonical WNT signaling in cancer stem cells and their niches: Cellular heterogeneity, omics reprogramming, targeted therapy and tumor plasticity (Review). Int J Oncol. 2017 Nov;51(5):1357-1369. doi: 10.3892/ijo.2017.4129. Epub 2017 Sep 19. Review. PubMed PMID: 29048660; PubMed Central PMCID: PMC5642388. 5: Katoh M. Multi-layered prevention and treatment of chronic inflammation, organ fibrosis and cancer associated with canonical WNT/β-catenin signaling activation (Review). Int J Mol Med. 2018 Aug;42(2):713-725. doi: 10.3892/ijmm.2018.3689. Epub 2018 May 17. PubMed PMID: 29786110; PubMed Central PMCID: PMC6034925.
Description: CWP232228, a highly potent selective Wnt/β-catenin signaling inhibitor, antagonizes binding of β-catenin to T-cell factor (TCF) in the nucleus. CWP232228 suppresses tumor formation and metastasis without toxicity through the inhibition of the growth of breast and liver cancer stem cells (CSCs)[1].
Target: Wnt/β-catenin[1]
In Vivo: CWP232228 (100 mg/kg, administered i.p.; daily; 21days for mice bearing 4T1 cell tumors; 60 days for mice bearing MDA-MB-435 cell tumors) results in a significant reduction in tumor volume[1]. Animal Model: 7-week-old female Balb/c and NOD/SCID mice bearing 4T1 or MDA-MB-435 cell tumors[1] Dosage: 100 mg/kg Administration: Administered i.p.; daily; 21days for mice bearing 4T1 cell tumors, 60 days for mice bearing MDA-MB-435 cell tumors Result: Treatment resulted in a significant reduction in tumor volume.
In Vitro: CWP232228 (0.01-100 μM; 48 hours) inhibits cell proliferation with IC50 values are 2 and 0.8 μM in mouse (4T1) and human (MDA-MB-435) breast cancer cell lines, respectively[1]. CWP232228 (0.01-10 μM; 48 hours) inhibits cell proliferation with IC50s of 2.566, 2.630, and 2.596 μM in Hep3B, Huh7 and HepG2 cells, respectively[2]. Cell Proliferation Assay[1] Cell Line: Mouse (4T1) and human (MDA-MB-435) breast cancer cell lines Concentration: 0.01, 0.1, 1, 10, 100 μM Incubation Time: 48 hours Result: IC50s were 2 and 0.8 μM for 4T1 and MDA-MB-435 cell lines, respectively. Cell Proliferation Assay[2] Cell Line: Hepatocellular carcinoma cell lines HepG2, Huh7, and Hep3B Concentration: 0.01, 0.1, 0.5, 1, 5, 10 μM Incubation Time: 48 hours Result: IC50s were 2.566, 2.630, and 2.596 μM for Hep3B, Huh7 and HepG2 cells, respectively.
References: [1]. Jang GB, et al. Wnt/β-Catenin Small-Molecule Inhibitor CWP232228 Preferentially Inhibits the Growth of Breast Cancer Stem-like Cells. Cancer Res. 2015 Apr 15;75(8):1691-702. [2]. Kim JY, et al. Oncotarget. 2016 Apr 12;7(15):20395-409. CWP232228 targets liver cancer stem cells through Wnt/β-catenin signaling: a novel therapeutic approach for liver cancer treatment.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
Cat. No. Product name Field of application
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