AZD3458

Name: AZD3458
Brand: MedChemExpress
SKU: HY-112443
Rating: 4.5 (1 reviews)

Cat. No.: HY-112443 Purity: 99.82%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

AZD3458 is a potent and remarkably selective PI3Kγ inhibitor with pIC₅₀s of 9.1, 5.1, <4.5, and 6.5 for PI3Kγ, PI3Kα, PI3Kβ, and PI3Kδ, respectively.

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

AZD3458 Chemical Structure

CAS No. : 2132961-46-5

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 275	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 275	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 250	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 425	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1530	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 2650	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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View All Isoforms

PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

Biological Activity
Purity & Documentation
References
Customer Review

Description

AZD3458 is a potent and remarkably selective PI3Kγ inhibitor with pIC₅₀s of 9.1, 5.1, <4.5, and 6.5 for PI3Kγ, PI3Kα, PI3Kβ, and PI3Kδ, respectively^[1].

IC₅₀ & Target^[1]

PI3Kγ

9.1 (pIC₅₀)

PI3Kα

5.1 (pIC₅₀)

PI3Kβ

4.5 (pIC₅₀)

PI3Kδ

6.5 (pIC₅₀)

PI3KC2α

5 (pIC₅₀)

PI3KC2β

7.5 (pIC₅₀)

PI3KC2γ

5.5 (pIC₅₀)

PI3KC3

5.1 (pIC₅₀)

In Vitro

AZD3458 (Compound 15) also inhibits PI3KC2α, PI3KC2β, PI3KC2γ, and PI3KC3 with pIC₅₀s of <5, 7.5, 5.5, and 5.1, respectively^[1].

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

Molecular Weight

433.54

Formula

C₂₀H₂₃N₃O₄S₂

CAS No.

2132961-46-5

Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C1N([C@@H](C)C2CC2)CC3=CC(C4=C(C)N=C(NC(C)=O)S4)=CC(S(=O)(C)=O)=C31

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 : 250 mg/mL (576.65 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	2.3066 mL	11.5330 mL	23.0659 mL
5 mM	0.4613 mL	2.3066 mL	4.6132 mL
10 mM	0.2307 mL	1.1533 mL	2.3066 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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.80 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.80 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (4.80 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

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: 99.82%

Select Batch:

Data Sheet (276 KB) SDS (251 KB)

COA (252 KB) HNMR (94 KB) LCMS (111 KB)

Handling Instructions (2659 KB)

References

[1]. Pemberton N, et al. Discovery of Highly Isoform Selective Orally Bioavailable Phosphoinositide 3-Kinase (PI3K)-γ Inhibitors. J Med Chem. 2018 Jun 28;61(12):5435-5441. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.3066 mL	11.5330 mL	23.0659 mL	57.6648 mL
	5 mM	0.4613 mL	2.3066 mL	4.6132 mL	11.5330 mL
	10 mM	0.2307 mL	1.1533 mL	2.3066 mL	5.7665 mL
	15 mM	0.1538 mL	0.7689 mL	1.5377 mL	3.8443 mL
	20 mM	0.1153 mL	0.5766 mL	1.1533 mL	2.8832 mL
	25 mM	0.0923 mL	0.4613 mL	0.9226 mL	2.3066 mL
	30 mM	0.0769 mL	0.3844 mL	0.7689 mL	1.9222 mL
	40 mM	0.0577 mL	0.2883 mL	0.5766 mL	1.4416 mL
	50 mM	0.0461 mL	0.2307 mL	0.4613 mL	1.1533 mL
	60 mM	0.0384 mL	0.1922 mL	0.3844 mL	0.9611 mL
	80 mM	0.0288 mL	0.1442 mL	0.2883 mL	0.7208 mL
	100 mM	0.0231 mL	0.1153 mL	0.2307 mL	0.5766 mL

AZD3458 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:

AZD34582132961-46-5AZD 3458AZD-3458PI3KPhosphoinositide 3-kinaseInhibitorinhibitorinhibit

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AZD3458

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AZD3458 Related Antibodies

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

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View All PI3K Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

AZD3458 Related Antibodies

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Dilution Calculator

Complete Stock Solution Preparation Table

AZD3458 Related Classifications

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Your Recently Viewed Products:

Customer Review

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