Taselisib (GDC 0032)

Synonyms: RG7604

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

Taselisib (GDC 0032) Chemical Structure

CAS: 1282512-48-4

Selleck's Taselisib (GDC 0032) has been cited by 32 publications

Purity & Quality Control

Batch: Purity: 99.97%
99.97

Taselisib (GDC 0032) Related Products

Signaling Pathway

Choose Selective PI3K Inhibitors

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human MOLM16 cells Proliferation assay 72 h Antiproliferative activity against human MOLM16 cells after 72 hrs by Cell Titer-Blue assay 22727640
Click to View More Cell Line Experimental Data

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
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]
Kinase Assay 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.
Experimental Result Images Methods Biomarkers Images 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
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]
Animal Research Animal Models MCF7-neo/Her2 xenograft model
Dosages 1.4, 2.8, 5.8, 11.25, or 22.5 mg/kg
Administration oral
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02785913 Completed
Recurrent Squamous Cell Lung Carcinoma|Stage IV Squamous Cell Lung Carcinoma
SWOG Cancer Research Network|National Cancer Institute (NCI)
November 2014 Phase 2
NCT01967966 Completed
Healthy Volunteer
Genentech Inc.
November 2013 Phase 1
NCT01814709 Completed
Healthy Volunteer
Genentech Inc.
April 2013 Phase 1

Chemical Information & Solubility

Molecular Weight 460.53 Formula

C24H28N8O2

CAS No. 1282512-48-4 SDF Download Taselisib (GDC 0032) SDF
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
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 70 mg/mL ( (151.99 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 7 mg/mL

Water : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

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

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy Taselisib (GDC 0032) | Taselisib (GDC 0032) supplier | purchase Taselisib (GDC 0032) | Taselisib (GDC 0032) cost | Taselisib (GDC 0032) manufacturer | order Taselisib (GDC 0032) | Taselisib (GDC 0032) distributor