[CAS NO. 1282514-88-8] GDC-0326

Name: GDC-0326
Brand: Arctom Scientific
SKU: SLK-S8157

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PRODUCTS SPECIFICATIONS [1282514-88-8]

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Catalog

SLK-S8157

Brand

Selleck

CAS

1282514-88-8

DESCRIPTION [1282514-88-8]

Overview

MDL	-
Molecular Weight	382.42
Molecular Formula	C19H22N6O3
SMILES	-

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.6149 mL	13.0746 mL	26.1493 mL
5 mM	0.5230 mL	2.6149 mL	5.2299 mL
10 mM	0.2615 mL	1.3075 mL	2.6149 mL
50 mM	0.0523 mL	0.2615 mL	0.5230 mL

Description

GDC-0326 is a potent and selective inhibitor of 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.

In vivo

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

References

[1] Heffron TP, et al. J Med Chem. 2016, 59(3):985-1002.
[2] Soler A, et al. Clin Cancer Res. 2016, 22(23):5805-5817.