Cat. No.: HY-153855

Zamaporvint

(Synonyms: RXC004)

Customer Review

Based on 1 Customer Validation

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.

Purity: 99.76%
CAS No.: 1900754-56-4
Formula: C₂₁H₁₆F₃N₇O
Molecular Weight:439.39

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Zamaporvint Chemical Structure

CAS No.: 1900754-56-4

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

All Wnt Isoforms :

All Acyltransferase Isoforms :

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 CL_int 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.

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)	C_max (p.o., μM)	C_{24 h} (p.o., μM)	AUC_inf (p.o., μM.h)	Cl (mL/min/kg)	V_ss (L/kg)	F (p.o., %)	T_1/2 (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

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

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

RXC004
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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

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Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2759 mL

11.3794 mL

22.7588 mL

5 mM

0.4552 mL

2.2759 mL

4.5518 mL

10 mM

0.2276 mL

1.1379 mL

2.2759 mL

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.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Dilution Calculator

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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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Zamaporvint

Metabolism/Protease Compound Library

Stem Cell Signaling Compound Library

Wnt/Hedgehog/Notch Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Differentiation Inducing Compound Library

Cytoskeleton Compound Library

Orally Active Compound Library

Neuroprotective Compound Library

Anti-Breast Cancer Compound Library

Lipid Metabolism Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Antihypertensive Compound Library

Metabolic Enzyme Compound Library

Highly Selective Inhibitors Library

Extracellular Vesicles (EVs) Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

Anti-Aging Compound Library Mini

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Fibrosis Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

All Wnt Isoforms

All Acyltransferase Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Zamaporvint Related Classifications

HY-153855 Related Classifications