2. Stem Cell/Wnt Metabolic Enzyme/Protease
  3. Wnt Acyltransferase Porcupine
  4. Zamaporvint

Zamaporvint  (Synonyms: RXC004)

Cat. No.: HY-153855 Purity: 99.76%
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Zamaporvint (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.

For research use only. We do not sell to patients.

Zamaporvint Chemical Structure

Zamaporvint Chemical Structure

CAS No. : 1900754-56-4

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 286 In-stock
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10 mM * 1 mL in DMSO USD 286 In-stock
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5 mg USD 260 In-stock
10 mg USD 420 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

Zamaporvint (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[1].

In Vitro

Zamaporvint (300 nM, 48 h) treatment of L- wnt3a cells reduce the ability of conditioned medium to activate the β-catenin-responsive luciferase reporter gene in a concentration-dependent manner, with an IC50 of 64 pM, and the addition of recombinant Wnt3a restore the luciferase activity, suggesting no effect on downstream Wnt signaling[1].
The effect of Zamaporvint (100 nM, 24 hr) on proliferation reflects a concentration-dependent downregulation of c-Myc mRNA. Reduced the proportion of cells in S phase and strongly suppressed the expression of the mitotic marker phospho-histone-H3 in cells with abnormal upstream components of the Wnt pathway, indicative of cell cycle arrest, and was found to have reduced immunosuppression at the same dose as after administration Sexual support[1] .
Zamaporvint (20 μM, 18 h) in plasma across species ranged from 2.5% to 7.5%, microsomal CLint values ranged from 3.9 to 31.6 μL/min?mg, with mouse having the lowest and dog the highest predicted clearances, rodents and humans display low clearance[1].
Zamaporvint (10 μM, 2 h) has good intrinsic permeability, showing some evidence of efflux in MDR1-MDCKII cells but not in Caco-2 cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Zamaporvint Related Antibodies

Western Blot Analysis[1]

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[1]

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.
In Vivo

Zamaporvint (1.5 mg/kg or 5 mg/kg orally twice daily, or 5 mg/kg Zamaporvint orally once daily, for 28 days) reduces 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, and no effected tumor growth in the Wnt ligand–independent HCT116 xenograft mode[1].
Zamaporvint (1.5 mg/kg, 5 mg/kg, once daily) reduces Ki67-positive cells in the total tumor area, and its effect is more pronounced in differentiated tumor areas, and by inhibiting immune evasion in the B16F10 "cold" tumor model Antitumor effect [1].
Zamaporvint (1.5 or 5 mg/kg once daily) stimulates host tumor immunity, reduces resident myeloid-derived suppressor cells within B16F10 tumors and synergizing with anti-programmed cell death protein-1 (PD-1, HY-P73361) to increase CD8+/regulatory T cell ratios within CT26 tumors[1].
Pharmacokinetic Parameters of Zamaporvint in Mice. [1]

species Dose (i.v./p.o., mg/kg) Cmax (p.o., μM) C24 h (p.o., μM) AUCinf (p.o., μM.h) Cl (mL/min/kg) Vss (L/kg) F (p.o., %) T1/2 (hr)
mouse 2/5 7.6 0.002 33.9 2.9 0.40 48 1.8
rat 2/5 3.6 0.009 10.5 5.8 0.64 31 2.5
dog 2/5 10.4 0.012 8.6 8.9 0.39 137 0.8

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: SCID-Beige mice were dosed at Translational Drug Discovery with vehicle[1]
Dosage: 1.5 mg/kg or 5 mg/kg; 5 mg/kg
Administration: 1.5 mg/kg or 5 mg/kg orally twice daily, or 5 mg/kg RXC004 orally once daily, for 28 days
Result: 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[1]
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 expression
Animal 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 mice[1]
Dosage: 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[1]
Dosage: 1.5 or 5 mg/kg (once daily).
Administration: p.o.
Result: Increased CD8+/regulatory T cell ratio.
Clinical Trial
Molecular Weight

439.39

Formula

C21H16F3N7O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(CN1C=NC(C2=CC(C(F)(F)F)=NC=C2)=C1C)NC3=NC=C(C4=CN=CC=N4)C=C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (284.49 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2759 mL 11.3794 mL 22.7588 mL
5 mM 0.4552 mL 2.2759 mL 4.5518 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation

Purity: 99.76%

COA (247 KB) HNMR (166 KB) LCMS (95 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2759 mL 11.3794 mL 22.7588 mL 56.8971 mL
5 mM 0.4552 mL 2.2759 mL 4.5518 mL 11.3794 mL
10 mM 0.2276 mL 1.1379 mL 2.2759 mL 5.6897 mL
15 mM 0.1517 mL 0.7586 mL 1.5173 mL 3.7931 mL
20 mM 0.1138 mL 0.5690 mL 1.1379 mL 2.8449 mL
25 mM 0.0910 mL 0.4552 mL 0.9104 mL 2.2759 mL
30 mM 0.0759 mL 0.3793 mL 0.7586 mL 1.8966 mL
40 mM 0.0569 mL 0.2845 mL 0.5690 mL 1.4224 mL
50 mM 0.0455 mL 0.2276 mL 0.4552 mL 1.1379 mL
60 mM 0.0379 mL 0.1897 mL 0.3793 mL 0.9483 mL
80 mM 0.0284 mL 0.1422 mL 0.2845 mL 0.7112 mL
100 mM 0.0228 mL 0.1138 mL 0.2276 mL 0.5690 mL
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Zamaporvint1900754-56-4RXC004RXC 004RXC-004WntAcyltransferasePorcupineDiacylglycerol acyltransferaseDiglyceride acyltransferaseacyl-CoA:cholesterol acyltransferasemono- acylglycerol acyltransferaseo-acyltransferase PorcupineinhibitorcolorectalpancreaticL- wnt3aXenograft ModelscancerInhibitorinhibit

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