Art. -Nr.: HY-139558

Zapnometinib

(Synonyms: PD0184264; ATR-002)

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Based on 1 Customer Validation

Zapnometinib (PD0184264), an active metabolite of CI-1040, is a MEK inhibitor, with an IC₅₀ of 5.7 nM. Zapnometinib exhibits antiviral activity against influenza virus and antibacterial activities.

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Reinheit: 99.85%
CAS. Nr.: 303175-44-2
Formel: C₁₃H₇ClF₂INO₂
Molecular Weight:409.55

Speicherung:

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Zapnometinib Chemical Structure

CAS. Nr.: 303175-44-2

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

MEK

5.7 nM (IC₅₀)

Alle MEK Isoform-spezifische Produkte anzeigen :

In Vitro

Zapnometinib (0.1 nM-1 μM) inhibits MEK, with IC₅₀s of 30.96 nM, 357 nM, and 15 nM in A549, MDCK cells and human PBMCs^[1].
Zapnometinib (100 μM; 4 h) inhibits the Ionomycin (PMA/I)-induced phosphorylation of ERK1/2 in human PBMCs^[1].
Zapnometinib (1-100 μM) reduces the viral titers of the IV H1N1pdm09, H3N2^[1].

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

Western Blot Analysis^[1]

Cell Line:

human PBMCs
Concentration:

100 μM
Incubation Time:

4 h
Result:

Inhibited the Ionomycin (PMA/I)-increased pERK1/2.

In Vivo

Zapnometinib (8.4-75 mg/kg/day; three times a day p.o.) reduces the lung virus titers and enhances survival of mice after lethal H1N1pdm09 infection^[1].
Zapnometinib (150 mg/kg) exhibits AUC values of 860.02 and 1953.68 μg h/mL in mice by i.v. or oral route, respectively^[1].

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

Animal Model:

Female C57BL/6 mice (8 weeks; 21-24 g) were infected with H1N1pdm09^[1]
Dosage:

8.4, 25, 75 mg/kg/day (2.8, 8.4, 25 mg/kg)
Administration:

P.o. three times a day
Result:

Significantly reduced the virus titer at the dose of either 75 mg/kg/day or 25 mg/kg/day.

Clinical Trial

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

Chemical Information

CAS. Nr. 303175-44-2
Appearance Solid
Molecular Weight 409.55
Formel C₁₃H₇ClF₂INO₂
Color Off-white to gray
SMILES

O=C(O)C1=CC=C(F)C(F)=C1NC2=CC=C(I)C=C2Cl
Synonyms

PD0184264; ATR-002
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 62.5 mg/mL (152.61 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

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.4417 mL

12.2085 mL

24.4170 mL

5 mM

0.4883 mL

2.4417 mL

4.8834 mL

10 mM

0.2442 mL

1.2209 mL

2.4417 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (5.08 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (5.08 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 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)

Verweise

[1]. Laure M, et, al. Antiviral efficacy against influenza virus and pharmacokinetic analysis of a novel MEK-inhibitor, ATR-002, in cell culture and in the mouse model. Antiviral Res. 2020 Jun;178:104806. [Content Brief]

[2]. Hamza H, et, al. Improved in vitro Efficacy of Baloxavir Marboxil Against Influenza A Virus Infection by Combination Treatment With the MEK Inhibitor ATR-002. Front Microbiol. 2021 Feb 12;12:611958. [Content Brief]

[3]. Bruchhagen C, et, al. Metabolic conversion of CI-1040 turns a cellular MEK-inhibitor into an antibacterial compound. Sci Rep. 2018 Jun 14;8(1):9114. [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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.4417 mL	12.2085 mL	24.4170 mL	61.0426 mL
	5 mM	0.4883 mL	2.4417 mL	4.8834 mL	12.2085 mL
	10 mM	0.2442 mL	1.2209 mL	2.4417 mL	6.1043 mL
	15 mM	0.1628 mL	0.8139 mL	1.6278 mL	4.0695 mL
	20 mM	0.1221 mL	0.6104 mL	1.2209 mL	3.0521 mL
	25 mM	0.0977 mL	0.4883 mL	0.9767 mL	2.4417 mL
	30 mM	0.0814 mL	0.4070 mL	0.8139 mL	2.0348 mL
	40 mM	0.0610 mL	0.3052 mL	0.6104 mL	1.5261 mL
	50 mM	0.0488 mL	0.2442 mL	0.4883 mL	1.2209 mL
	60 mM	0.0407 mL	0.2035 mL	0.4070 mL	1.0174 mL
	80 mM	0.0305 mL	0.1526 mL	0.3052 mL	0.7630 mL
	100 mM	0.0244 mL	0.1221 mL	0.2442 mL	0.6104 mL

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Zapnometinib

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Alle MEK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Zapnometinib Related Classifications

HY-139558 Related Classifications