Home Tools

Zamaporvint

Catalog No. T77780 CAS 1900754-56-4

Synonyms: RXC004

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.Zamaporvint has shown anti-tumor and anti-proliferative activity in a wide range of cancer cell lines.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

Zamaporvint, CAS 1900754-56-4

Pack Size	Availability	Price/USD
1 mg	In stock	$ 87.00
5 mg	In stock	$ 213.00
10 mg	In stock	$ 347.00
25 mg	In stock	$ 690.00
50 mg	In stock	$ 1,120.00
1 mL * 10 mM (in DMSO)	In stock	$ 235.00

Bulk Inquiry

Select Batch

Purity: 97.5%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	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.Zamaporvint has shown anti-tumor and anti-proliferative activity in a wide range of cancer cell lines.
Targets&IC50	L-wnt3a cells:64 pM
In vitro	Treatment of L-wnt3a cells with Zamaporvint (300 nM, 48 h) dose-dependently reduced the ability to activate β-catenin responsive luciferase reporter gene in conditioned medium, with an IC50 of 64 pM. The addition of recombinant Wnt3a restored luciferase activity, indicating no impact on downstream Wnt signaling transduction[1].The impact of Zamaporvint (100 nM, 24 h) on proliferation reflected a concentration-dependent downregulation of c-Myc mRNA. There was a decrease in the proportion of cells in the S phase, and a strong inhibition of the expression of mitotic marker phosphorylated histone-H3 in cells with aberrant upstream Wnt pathway components, suggesting cell cycle arrest. Additionally, an additive effect was observed at the same dose, revealing a reduction in its immunosuppressive properties after administration[1].
In vivo	Zamaporvint, administered orally at doses of 1.5 mg/kg or 5 mg/kg twice daily, or 5 mg/kg once daily for 28 days, has demonstrated the ability to reduce tumor growth. In ligand-dependent SNU-1411, AsPC1, and HPAF II models with observable inhibition of Wnt-responsive gene expression (including cMyc), as well as in Wnt ligand-independent HCT116 xenograft models, tumor growth remained unaffected[1].At a dose of 1.5 mg/kg and 5 mg/kg once daily, Zamaporvint reduced the number of Ki67-positive cells in the overall tumor area, with a more pronounced effect in the differentiated tumor regions. Its anti-tumor effects were observed in the B16F10 "cold" tumor model through the inhibition of immune evasion[1].Zamaporvint, at doses of 1.5 or 5 mg/kg once daily, stimulated the host tumor immune response by decreasing bone marrow-derived suppressor cells within B16F10 tumors. It also exhibited a synergistic effect with anti-programmed cell death protein-1 (PD-1) to increase the proportion of regulatory T cells (CD8+/CT26) within the tumor[1].

Synonyms	RXC004
Molecular Weight	439.39
Formula	C21H16F3N7O
CAS No.	1900754-56-4

Storage

store at low temperature,keep away from direct sunlight

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL (227.59 mM), Sonication is recommended.

References and Literature

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.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library

Dose Conversion

You can also refer to dose conversion for different animals. More

In vivo Formulation Calculator (Clear solution)

Step One: Enter information below

Dosage

mg/kg

Average weight of animals

Dosing volume per animal

Number of animals

Step Two: Enter the in vivo formulation

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

Calculate Reset

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid 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 master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

Note:

Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Calculator

Molarity Calculator

Dilution Calculator

Reconstitution Calculation

Molecular Weight Calculator

Mass

Concentration

Volume

Molecular Weight

Molarity Calculator allows you to calculate the

Mass of a compound required to prepare a solution of known volume and concentration
Volume of solution required to dissolve a compound of known mass to a desired concentration
Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

Molecule Formula

Molecular Weight g/mol

Enter the chemical formula of a compound to calculate its molar mass and elemental composition

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

bottom

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Zamaporvint 1900754-56-4 Others RXC004 RXC-004 RXC 004 inhibitor inhibit

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.