
Zamaporvint
CAS No. 1900754-56-4
Zamaporvint( —— )
Catalog No. M37117 CAS No. 1900754-56-4
Zamaporvint (RXC004) is a selective, orally active and potent inhibitor of the Wnt pathway that acts on the membrane-bound fatty acyltransferase porcupine to block Wnt ligand palmitoylation, secretion, and pathway activation.
Purity : >98% (HPLC)






Size | Price / USD | Stock | Quantity |
2MG | 132 | Get Quote |
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5MG | 202 | Get Quote |
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10MG | 330 | Get Quote |
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25MG | 635 | Get Quote |
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50MG | 1030 | Get Quote |
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500MG | Get Quote | Get Quote |
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1G | Get Quote | Get Quote |
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Biological Information
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Product NameZamaporvint
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NoteResearch use only, not for human use.
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Brief DescriptionZamaporvint (RXC004) is a selective, orally active and potent inhibitor of the Wnt pathway that acts on the membrane-bound fatty acyltransferase porcupine to block Wnt ligand palmitoylation, secretion, and pathway activation.
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DescriptionZamaporvint (RXC004) is an orally active and selective inhibitor of Wnt. Zamaporvint targete membrane-bound o-acyltransferase Porcupine and inhibited Wnt ligand palmitoylation, secretion, and pathway activation. Zamaporvint displays a favorable pharmacokinetic profile and shows potent antiproliferative effects in Wnt ligand-dependent colorectal and pancreatic cell lines. Zamaporvint possesses multiple antitumor mechanisms and can be used in cancer research.
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In VitroWestern Blot Analysis Cell Line:L-Wnt5a Concentration:300 nM Incubation Time:48 h Result:Activated the β-catenin-responsive luciferase reporter gene in a concentration-dependent manner, with an IC50 of 64 pmol/L.Apoptosis Analysis Cell Line: L-Wnt5a Concentration:100 nM Incubation Time:24 h Result:Downregulated c-Myc mRNA and reduce the proportion of cells in S-phase, and strongly inhibited expression of the mitosis marker phospho-histone-H3 in cells with upstream aberrations in Wnt pathway components.
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In VivoAnimal Model:SCID-Beige mice were dosed at Translational Drug Discovery with vehicleDosage:1.5 mg/kg or 5 mg/kg; 5 mg/kgAdministration:1.5 mg/kg or 5 mg/kg orally twice daily, or 5 mg/kg RXC004 orally once daily, for 28 daysResult:Reduced in tumor growth, and inhibition of Wnt-responsive gene expression including cMyc, was observed in the Wnt ligand–dependent SNU-1411, AsPC1, and HPAFII models.No effected tumor growth in the Wnt ligand–independent HCT116 xenograft mode.Animal Model:HPAF-II (5 × 106 cells; athymic nude mice), AsPC1 (3 × 106 cells; athymic nude mice), and SNU-1411 (1×107 cells; NOD-SCID mice) were implanted bilaterally, subcutaneously, whereas HCT116 (3 × 106 cells; athymic nude mice) were implanted in a single flank Dosage:Dosing was either 1.5 mg/kg twice daily RXC004 for 7–13 days then once daily for the remainder of study (up to 29 days), or 28 days 1.5 mg/kg twice daily RXC004 for HCT116 Administration:p.o.Result:Demonstrated to inhibit tumor growth and Wnt-responsive gene expressionAnimal Model:B16F10/C57BL/6 syngeneic model was performed at Axis Bioservices. Mouse B16F10 cells (2 × 105) were subcutaneously implanted in flanks of the immunocompetent male C57BL/6 miceDosage:5 mg/kg once daily Administration: p.o.Result: Inhibited tumor growth and improved model survival.Animal Model:CT26/BALB/c syngeneic model was performed at ProQuinase GmbH. Mouse CT26 cells (5 × 105) were subcutaneously implanted in the flanks of the immunocompetent female BALB/c mice Dosage:1.5 or 5 mg/kg (once daily).Administration:p.o.Result:Increased CD8+/regulatory T cell ratio.
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Synonyms——
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PathwayOthers
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TargetOther Targets
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RecptorOthers
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Research Area——
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Indication——
Chemical Information
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CAS Number1900754-56-4
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Formula Weight439.39
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Molecular FormulaC21H16F3N7O
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Purity>98% (HPLC)
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SolubilityIn Vitro:?DMSO : 125 mg/mL (284.49 mM; Ultrasonic )
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SMILESO=C(NC1=NC=C(C=C1)C=2N=CC=NC2)CN3C=NC(C=4C=CN=C(C4)C(F)(F)F)=C3C
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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Phillips C, The Wnt Pathway Inhibitor RXC004 Blocks Tumor Growth and Reverses Immune Evasion in Wnt Ligand-dependent Cancer Models. Cancer Res Commun. 2022 Sep 2;2(9):914-928.?
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