GDC-0326

Catalog No.S8157 Batch:S815701

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Technical Data

Formula

C19H22N6O3
Molecular Weight 382.42 CAS No. 1282514-88-8
Solubility (25°C)* In vitro DMSO 76 mg/mL (198.73 mM)
Ethanol 19 mg/mL (49.68 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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 Assay:

[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 Study:

[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.

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

Idelalisib Rescues Natural Killer Cells from Monocyte-Induced Immunosuppression by Inhibiting NOX2-Derived Reactive Oxygen Species [ Cancer Immunol Res, 2020, 8(12):1532-1541] PubMed: 32967913
A humanized yeast-based toolkit for monitoring phosphatidylinositol 3-kinase activity at both single cell and population levels [Coronas-Serna JM Microb Cell, 2018, ;5(12):545-554] PubMed: 30533419

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.