Taselisib

Taselisib (GDC-0032) is a potent PI3K inhibitor targets PIK3CA mutations, with Kis of 0.12 nM, 0.29 nM, 0.97 nM, and 9.1 nM for PI3Kδ, PI3Kα, PI3Kγ and PI3Kβ, respectively.

Product Specifications

CAS Number

[1282512-48-4]

Product Name Alternative

GDC-0032; RG-7604

UNSPSC

12352005

Hazard Statement

H302, H312, H332

Target

PI3K

Type

Reference compound

Related Pathways

PI3K/Akt/mTOR

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/GDC-0032.html

Purity

99.75

Solubility

DMSO : 25 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

CC(C)N1C(C2=CN3C(C(C(OCC3)=C4)=CC=C4C5=CN(C(C)(C(N)=O)C)N=C5)=N2)=NC(C)=N1

Molecular Formula

C24H28N8O2

Molecular Weight

460.53

Precautions

H302, H312, H332

References & Citations

[1]Zachary S. Zumsteg, et al. Taselisib (GDC-0032), a Potent β-Sparing Small Molecule Inhibitor of PI3K, Radiosensitizes Head and Neck Squamous Carcinomas Containing Activating PIK3CA Alterations. Clin Cancer Res. 2016 Apr 15; 22 (8) : 2009–2019.|[2]Marian M. Deuker, et al. PI3′-Kinase Inhibition Forestalls the Onset of MEK1/2 Inhibitor Resistance in BRAF-Mutated Melanoma. Cancer Discov. 2015 Feb; 5 (2) : 143–153.|[3]Ndubaku CO, et al. Discovery of 2-{3-[2- (1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl) -5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032) : a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust in vivo antitumor activity. J Med Chem. 2013 Jun 13;56 (11) :4597-610.