Home PI3K/Akt/mTOR PI3K inhibitor GDC-0326 For research use only.

GDC-0326

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

GDC-0326 Chemical Structure

CAS No. 1282514-88-8

Purity & Quality Control

Batch: S815701 DMSO]76 mg/mL]false]Ethanol]19 mg/mL]false]Water]Insoluble]false Purity: 99.84%
99.84

GDC-0326 Related Products

Signaling Pathway

PI3K Signaling Pathways

PI3K Signaling Pathway

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

Chemical Information & Solubility

Molecular Weight 382.42 Formula

C19H22N6O3
CAS No. 1282514-88-8 SDF Download GDC-0326 SDF
Smiles CC(C)N1C(=NC=N1)C2=CN3CCOC4=C(C3=N2)C=CC(=C4)OC(C)C(=O)N
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 76 mg/mL ( (198.73 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 19 mg/mL

Water : Insoluble


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In vivo
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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.

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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