GDC-0326

Catalog No.S8157

For research use only.

GDC-0326 is a potent and selective inhibitor of PI3Kα with Ki value of 0.2 nM; remarkably selective over the other class I isoforms in enzymatic assays.

GDC-0326 Chemical Structure

CAS No. 1282514-88-8

Selleck's GDC-0326 has been cited by 2 Publications

Purity & Quality Control

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Biological Activity

Description GDC-0326 is a potent and selective inhibitor of PI3Kα with Ki value of 0.2 nM; remarkably selective over the other class I isoforms in enzymatic assays.
Targets
PI3Kα [1]
(Cell-free assay)
PI3Kδ [1]
(Cell-free assay)
PI3Kγ [1]
(Cell-free assay)
PI3Kβ [1]
(Cell-free assay)
0.2 nM(Ki) 4 nM(Ki) 10.2 nM(Ki) 26.6 nM(Ki)
In vitro

In addition to achieving selectivity over the other class I isoforms, the PI3Kα specific inhibitor GDC-0326 also achieves a very high level of selectivity over other kinases. GDC-0326 is not an inhibitor of cytochrome P450 enzymes tested[1].

In vivo GDC-0326 has consistently low clearance and high oral bioavailability across species tested, enabling significant sustained free drug levels[1].

Protocol (from reference)

Cell Research:

[2]

  • Cell lines: βTC3 cells
  • Concentrations: 1 μM
  • Incubation Time: 2 h
  • Method:

    βTC3 cells are plated at 1 × 106 per dish. 24 h later, cells are treated for 2 h with vehicle, GDC-0941 (1 μM), GDC-0326 (1 μM), TGX-221 (0.5 μM), IC87114 (5 μM), BKM120 (0.8 μM) or BYL719 (1 μM) and lysed. 

Animal Research:

[1]

  • Animal Models: Nude (MCF7-neo/HER2) and scid beige (KPL-4) mice
  • Dosages: 0.78, 1.56, 3.25, 6.25, or 12.5 mg/kg
  • Administration: p.o.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 382.42
Formula

C19H22N6O3

CAS No. 1282514-88-8
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C)N1C(=NC=N1)C2=CN3CCOC4=C(C3=N2)C=CC(=C4)OC(C)C(=O)N

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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