Home PI3K/Akt/mTOR PI3K inhibitor Taselisib (GDC 0032)

Taselisib (GDC 0032)

Catalog No.S7103 Synonyms: RG7604

For research use only.

Taselisib (GDC 0032, RG7604) is a potent, next-generation β isoform-sparing PI3K inhibitor targeting PI3Kα/δ/γ with Ki of 0.29 nM/0.12 nM/0.97nM, >10 fold selective over PI3Kβ.

Taselisib (GDC 0032) Chemical Structure

CAS No. 1282512-48-4

Selleck's Taselisib (GDC 0032) has been cited by 18 publications

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Biological Activity

Description Taselisib (GDC 0032, RG7604) is a potent, next-generation β isoform-sparing PI3K inhibitor targeting PI3Kα/δ/γ with Ki of 0.29 nM/0.12 nM/0.97nM, >10 fold selective over PI3Kβ.
Features A beta isoform-sparing PI3K inhibitor.
Targets
PI3Kδ [1]
(Cell-free assay)		 PI3Kα [1]
(Cell-free assay)		 PI3Kγ [1]
(Cell-free assay)		 PI3Kβ [1]
(Cell-free assay)		 C2β [1]
(Cell-free assay)		 Click to View More Targets
0.12 nM(Ki) 0.29 nM(Ki) 0.97 nM(Ki) 9.1 nM(Ki) 292 nM
In vitro

GDC-0032 is an orally bioavailable, potent, and selective inhibitor of Class I PI3Kα, δ, and γ isoforms, with 30 fold less inhibition of the PI3K β isoform relative to the PI3Kα isoform. Preclinical data show that GDC-0032 has increased activity against PI3Kα isoform (PIK3CA) mutant and HER2-amplified cancer cell lines. GDC-0032 inhibits MCF7-neo/HER2 cells proliferation with IC50 of 2.5 nM. [1]
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human MOLM16 cells NVuwd3l4WHKxbHnm[ZJifGmxbjDhd5NigQ>? NXrZZ4hOPzJiaB?= MnnmRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPT1zNNVYh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IFPlcIwhXGm2ZYKtRox2\SCjc4PhfS=> MWOyNlczPzZ2MB?=
Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot Cyclin D1 / Cyclin E / Cleaved PARP / p-AKT / pPRAS40 / p-mTOR / pp70S6K / BRCA1 / c-Myc 27382432
Growth inhibition assay Cell viability 27382432
In vivo GDC-0032 pharmacokinetics is approximately dose proportional and time independent with a mean t1/2 of 40 hours. The combination of GDC-0032 enhances activity of fulvestrant resulting in tumor regressions and tumor growth delay (91% tumor growth inhibition (TGI)). In addition, the combination of GDC-0032 with tamoxifen enhances the efficacy of tamoxifen in vivo (102%TGI for GDC-0032). [1]

Protocol (from reference)

Kinase Assay:[1]
  • Characterization of Biochemical and Cellular Activity in Vitro:

    Enzymatic activity of the class I PI3K isoforms is measured using a fluorescence polarization assay that monitors formation of the product 3,4,5-inositoltriphosphate molecule as it competes with fluorescently labeled PIP3 for binding to the GRP-1 pleckstrin homology domain protein. An increase in phosphatidyl inositide-3-phosphate product results in a decrease in fluorescence polarization signal as the labeled fluorophore is displaced from the GRP-1 protein binding site. Class I PI3K isoforms are expressed and purified as heterodimeric recombinant proteins. Tetramethylrhodamine-labeled PIP3 (TAMRA-PIP3), di-C8-PIP2, and PIP3 detection reagents are purchased from Echelon Biosciences. PI3Kα is assayed under initial rate conditions in the presence of 10 mM Tris (pH 7.5), 25 μM ATP, 9.75 μM PIP2, 5% glycerol, 4 mM MgCl2, 50 mM NaCl, 0.05% (v/v) Chaps, 1 mM dithiothreitol, and 2% (v/v) DMSO at 60 ng/mL. After assay for 30 min at 25 °C, reactions are terminated with a final concentration of 9 mM EDTA, 4.5 nM TAMRA-PIP3, and 4.2 μg/mL GRP-1 detector protein before reading fluorescence polarization on an Envision plate reader. IC50 values are calculated from the fit of the dose-response curves to a 4-parameter equation. Each reported value is an average of three experiments, and all have a standard deviation less than one geometric mean.
Animal Research:[1]
  • Animal Models: MCF7-neo/Her2 xenograft model
  • Dosages: 1.4, 2.8, 5.8, 11.25, or 22.5 mg/kg
  • Administration: oral
  • (Only for Reference)

Solubility (25°C)

In vitro

 DMSO 70 mg/mL warmed
(151.99 mM)
Water Insoluble
Ethanol 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.

Chemical Information

Molecular Weight 460.53
Formula

C24H28N8O2
CAS No. 1282512-48-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=NN(C(=N1)C2=CN3CCOC4=C(C3=N2)C=CC(=C4)C5=CN(N=C5)C(C)(C)C(=O)N)C(C)C

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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.
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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02785913 Completed Other: Laboratory Biomarker Analysis|Drug: Taselisib Recurrent Squamous Cell Lung Carcinoma|Stage IV Squamous Cell Lung Carcinoma Southwest Oncology Group|National Cancer Institute (NCI) November 2014 Phase 2
NCT01967966 Completed Drug: GDC-0032 Healthy Volunteer Genentech Inc. November 2013 Phase 1
NCT01814709 Completed Drug: GDC-0032|Drug: Itraconazole|Drug: Rifampin Healthy Volunteer Genentech Inc. April 2013 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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.

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