Deltazinone 1

Name: Deltazinone 1
Brand: MedChemExpress
SKU: HY-108436
Rating: 4.5 (1 reviews)

Cat. No.: HY-108436 Purity: 98.79%: Data Sheet
COA

SDS
Handling Instructions
FAQs
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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.

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

Deltazinone 1 Chemical Structure

CAS No. : 894554-89-3

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	Get quote
200 mg	Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE7 PDE9 PDE10 PDE11 PDE12 PDE8 Autotaxin

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[2]

PDEδ

8 nM (Kd)

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.

Molecular Weight

457.57

Formula

C₂₇H₃₁N₅O₂

CAS No.

894554-89-3

Appearance

Solid

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

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 : 100 mg/mL (218.55 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	2.1855 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

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.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 98.79%

Select Batch:

Data Sheet (271 KB) SDS (251 KB)

COA (244 KB) HNMR (263 KB) LCMS (103 KB)

Handling Instructions (2659 KB)

References

[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]

Complete Stock Solution Preparation Table

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

Deltazinone 1 Related Classifications

Help & FAQs

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:

Deltazinone 1894554-89-3Deltazinone1Deltazinone-1Phosphodiesterase (PDE)pyrazolopyridazinonePDEδPDEδ-RasKRasPanc-Tu-IMIA PaCa-2Capan-1S6PInhibitorinhibitorinhibit

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Deltazinone 1

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Complete Stock Solution Preparation Table

Deltazinone 1 Related Classifications

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