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GDC-0326

Name: GDC-0326
Brand: TargetMol
SKU: T3985
Price: 30 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T3985Cas No. 1282514-88-8

Alias GDC0326, GDC 0326

GDC-0326 is a potent and selective inhibitor of the α-isoform of Phosphoinositide 3-Kinase (PI3Kalpha inhibitor).

GDC-0326

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Purity: 99.35%

Catalog No. T3985Alias GDC0326, GDC 0326Cas No. 1282514-88-8

GDC-0326 is a potent and selective inhibitor of the α-isoform of Phosphoinositide 3-Kinase (PI3Kalpha inhibitor).

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$30	In Stock	In Stock
2 mg	$45	In Stock	In Stock
5 mg	$87	In Stock	In Stock
10 mg	$157	In Stock	In Stock
25 mg	$268	In Stock	In Stock
50 mg	$428	In Stock	In Stock
100 mg	$623	-	In Stock
1 mL x 10 mM (in DMSO)	$95	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Batch Information

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Purity:99.35%

Appearance:Solid

Color:White

Resource Download

COA HNMR HPLC LCMS

Product Introduction

GDC-0326 AI Summary

GDC-0326 exhibits a range of bioactivities, including high inhibitory activity against multiple Cytochrome P450 enzymes (CYP3A4, CYP2C9, CYP1A2, CYP2C19, and CYP2D6) with IC50 values greater than 10000.0 nM. It has good apparent permeability in MDCK cells and moderate selectivity for PI3K isoforms. The compound demonstrates antiproliferative activity against MCF7-neo/Her2 cells and PC3 cells with EC50 values of 100.0 nM and 2200.0 nM, respectively, and cytotoxicity against KPL4 cells with an EC50 value of 60.0 nM. GDC-0326 displays significant antitumor activity in xenografted mouse models, with tumor growth inhibition ranging from 73.0% to 110.0% at varying doses, and decreases phosphorylated Akt levels in MCF7-neo/Her2 xenografted mice. It shows potent inhibition of PI3Kalpha with a Ki value of 0.2 nM and notable selectivity for PI3Kalpha over PI3Kdelta (ratio Ki of 22.0). It inhibits the H1047R mutant of PI3Kalpha in human HCC1954 cells, reducing PRAS40 phosphorylation with an EC50 of 89.0 nM, and has slight selectivity for mutant over wild type PI3Kalpha (ratio EC50 of 1.4). Also, the compound inhibits PI3Kdelta in human B-cells, reducing CD69 expression with an IC90 of 147.0 nM and demonstrates low toxicity, indicated by minimal body weight loss in toxicity assays. Its lipophilicity, measured as LogD in 1-Octanol/PBS at pH 7.4, is 1.9. GDC-0326 has good oral bioavailability and plasma protein binding across different animal models..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	GDC-0326 is a potent and selective inhibitor of the α-isoform of Phosphoinositide 3-Kinase (PI3Kalpha inhibitor).
Targets&IC50	PI3Kα:0.2 nM(Ki), PI3Kγ:10.2 nM(Ki), PI3Kβ:26.6 nM(Ki), PI3Kδ:4 nM(Ki)
Synonyms	GDC0326, GDC 0326

Chemical Properties

Molecular Weight	382.42
Formula	C₁₉H₂₂N₆O₃
Cas No.	1282514-88-8
Smiles	CC(C)n1ncnc1-c1cn2CCOc3cc(O[C@@H](C)C(N)=O)ccc3-c2n1
Relative Density.	1.44 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 69 mg/mL (180.43 mM), Sonication is recommended.

H2O: Insoluble

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.23 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.6149 mL	13.0746 mL	26.1493 mL	130.7463 mL
5 mM	0.5230 mL	2.6149 mL	5.2299 mL	26.1493 mL
10 mM	0.2615 mL	1.3075 mL	2.6149 mL	13.0746 mL
20 mM	0.1307 mL	0.6537 mL	1.3075 mL	6.5373 mL
50 mM	0.0523 mL	0.2615 mL	0.5230 mL	2.6149 mL
100 mM	0.0261 mL	0.1307 mL	0.2615 mL	1.3075 mL

Calculator

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc