Art. -Nr.: HY-108436

Deltazinone 1

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Deltazinone 1, a pyrazolopyridazinone, is a highly selective PDEδ inhibitor with a K_D of 8 nM. Deltazinone 1 inhibits the PDEδ-Ras interaction. Deltazinone 1 shows a dose-dependent inhibitory response on proliferation in oncogenic KRas-dependent cell lines.

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Reinheit: 98.79%
CAS. Nr.: 894554-89-3
Formel: C₂₇H₃₁N₅O₂
Molecular Weight:457.57

Speicherung:

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

Deltazinone 1 Chemical Structure

CAS. Nr.: 894554-89-3

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

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[2]

PDEδ

8 nM (Kd)

Alle Phosphodiesterase (PDE) Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
CAPAN-1	IC₅₀	48 μM Compound: 2	Antiproliferative activity against KRAS-dependent human Capan1 cells after 48 hrs by CCK8 assay Antiproliferative activity against KRAS-dependent human Capan1 cells after 48 hrs by CCK8 assay	[PMID: 29510040]
CAPAN-1	IC₅₀	56.9 μM Compound: S2	Antiproliferative activity against KRAS-dependent human Capan1 cells after 48 hrs by CCK8 assay Antiproliferative activity against KRAS-dependent human Capan1 cells after 48 hrs by CCK8 assay	[PMID: 28929751]
HCT-116	IC₅₀	74 μM Compound: 2	Antiproliferative activity against human HCT116 cells incubated for 72 hrs by CCK8 assay Antiproliferative activity against human HCT116 cells incubated for 72 hrs by CCK8 assay	[PMID: 32603594]
HCT-116	IC₅₀	82.4 μM Compound: 1	Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition and measured after 72 hrs by CCK8 assay Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition and measured after 72 hrs by CCK8 assay	[PMID: 35178186]
SW480	IC₅₀	18.3 μM Compound: 1	Antiproliferative activity against human SW480 cells assessed as cell growth inhibition and measured after 72 hrs by CCK8 assay Antiproliferative activity against human SW480 cells assessed as cell growth inhibition and measured after 72 hrs by CCK8 assay	[PMID: 35178186]
SW480	IC₅₀	56 μM Compound: 2	Antiproliferative activity against human SW480 cells incubated for 72 hrs by CCK8 assay Antiproliferative activity against human SW480 cells incubated for 72 hrs by CCK8 assay	[PMID: 32603594]

In Vitro

Deltazinone 1 (0.375-24 μM; 0-120 h) inhibits cell growth in a dose-dependent manner^[1].
Deltazinone 1 (20 μM; 1 h) reduces S6P phosphorylation in the KRas-dependent Panc-Tu-I cells^[1].
Deltazinone 1 (10 μM) shows cell death for oncogenic KRas-dependent Panc-Tu-I cells but not for oncogenic KRas-independent PANC-1 cells^[1].

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

Cell Viability Assay^[1]

Cell Line:

Panc-Tu-I, MIA PaCa-2, Capan-1 cells
Concentration:

0.375, 0.75, 1.5, 3, 6, 12, 24 μM
Incubation Time:

0-120 h
Result:

Inhibited cell growth in a dose-dependent manner already observable at sub-μM concentrations.
At doses higher than 3 μM decreasing cell indices indicated cell death ∼30 h in Panc-Tu-I cells and after ∼40 h in MIA PaCa-2.
Doses up to 24 μM led to strong growth inhibition but not cell death in the Capan-1 cell line.

Western Blot Analysis^[1]

Cell Line:

Panc-Tu-I cells
Concentration:

20 μM
Incubation Time:

1 h
Result:

Reduced S6P phosphorylation in the KRas-dependent Panc-Tu-I cells.
Did not significantly affect Erk response to EGF.

Chemical Information

CAS. Nr. 894554-89-3
Appearance Solid
Molecular Weight 457.57
Formel C₂₇H₃₁N₅O₂
Color White to off-white
SMILES

CC1=CC=C(N2C(C)=C(C(C)=NN(CCCC(NCC(C)C3=CC=CC=C3)=O)C4=O)C4=N2)C=C1
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (218.55 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

2.1855 mL

10.9273 mL

21.8546 mL

5 mM

0.4371 mL

2.1855 mL

4.3709 mL

10 mM

0.2185 mL

1.0927 mL

2.1855 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.

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 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.46 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 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 (271 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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]. Björn Papke, et al. Identification of pyrazolopyridazinones as PDEδ inhibitors. Nat Commun. 2016 Apr 20;7:11360. [Content Brief]

[2]. Pablo Martín-Gago, et al. Structure-based development of PDEδ inhibitors. Biol Chem. 2017 May 1;398(5-6):535-545. [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	2.1855 mL	10.9273 mL	21.8546 mL	54.6364 mL
	5 mM	0.4371 mL	2.1855 mL	4.3709 mL	10.9273 mL
	10 mM	0.2185 mL	1.0927 mL	2.1855 mL	5.4636 mL
	15 mM	0.1457 mL	0.7285 mL	1.4570 mL	3.6424 mL
	20 mM	0.1093 mL	0.5464 mL	1.0927 mL	2.7318 mL
	25 mM	0.0874 mL	0.4371 mL	0.8742 mL	2.1855 mL
	30 mM	0.0728 mL	0.3642 mL	0.7285 mL	1.8212 mL
	40 mM	0.0546 mL	0.2732 mL	0.5464 mL	1.3659 mL
	50 mM	0.0437 mL	0.2185 mL	0.4371 mL	1.0927 mL
	60 mM	0.0364 mL	0.1821 mL	0.3642 mL	0.9106 mL
	80 mM	0.0273 mL	0.1366 mL	0.2732 mL	0.6830 mL
	100 mM	0.0219 mL	0.1093 mL	0.2185 mL	0.5464 mL

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Deltazinone 1

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Anti-Alzheimer's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Anti-Colorectal Cancer Compound Library

Metabolic Enzyme Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Alle Phosphodiesterase (PDE) Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Deltazinone 1

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Anti-Alzheimer's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Anti-Colorectal Cancer Compound Library

Metabolic Enzyme Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Alle Phosphodiesterase (PDE) Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Deltazinone 1 Related Classifications

HY-108436 Related Classifications