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Taselisib (GDC 0032)

Name: Taselisib (GDC 0032)
Brand: Selleck Chemicals
SKU: S7103
Rating: 5 (38 reviews)

Synonyms: RG7604

Catalog No.S7103 Purity:99.97%

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

Taselisib (GDC 0032) Chemical Structure

CAS No. 1282512-48-4

Purity & Quality Control

Batch: Purity: 99.97%

99.97

Taselisib (GDC 0032) Related Products

Related Targets	p110α p110β p110δ p110γ C2β Vps34	Click to Expand
Related Products	LY294002 3-MA (3-Methyladenine) Dactolisib (BEZ235) Pictilisib (GDC-0941) Wortmannin Buparlisib (BKM120) PI-103 TGX-221 ZSTK474 Omipalisib (GSK2126458) A66 PF-04691502 PIK-75 HCl IC-87114 740 Y-P (PDGFR 740Y-P) AS-605240 SAR405 Apitolisib (GDC-0980) VPS34-IN1 PIK-90 AZD6482 Gedatolisib (PKI-587) HS-173 AS-252424 Eganelisib (IPI-549) VS-5584 (SB2343) GSK2636771 AZD8186 GSK1059615 Pilaralisib (XL147) TG100-115 CZC24832 Voxtalisib (XL765) XL147 analogue AS-604850 BGT226 (NVP-BGT226) maleate Quercetin Dihydrate VPS34 inhibitor 1 (Compound 19) Samotolisib (LY3023414) Voxtalisib (XL765) Analogue AMG319 Nemiralisib Bimiralisib (PQR309) CH5132799 PKI-402 TG100713 Paxalisib (GDC-0084) SF2523 Serabelisib (TAK-117) GDC-0326 GNE-317 Inavolisib (GDC-0077) PIK-294 PI-3065 AZD8835 Seletalisib (UCB-5857) leniolisib (CDZ 173) (E)-Akt inhibitor-IV Gallein CAY10505 Selective PI3Kδ Inhibitor 1 (compound 7n) PF-4989216 GNE-477 GNE-493	Click to Expand
Related Compound Libraries	Kinase Inhibitor Library PI3K/Akt Inhibitor Library Apoptosis Compound Library Cell Cycle compound library NF-κB Signaling Compound Library	Click to Expand

Signaling Pathway

PI3K Signaling Pathway

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 K_i 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	Click to View More Targets

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
Kinase Assay	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 t_1/2 of 40 hours. The combination of GDC-0032 enhances activity resulting in tumor regressions and tumor growth delay (91% tumor growth inhibition (TGI)). In addition, the combination of GDC-0032 enhances the efficacy 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
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-05-22)
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

References

[1] Ndubaku CO, et al. J Med Chem, 2013, 56(11), 4597-4610.

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)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

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
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.600mg/ml (9.99mM)	Taking the 1 mL working solution as an example, add 50 μL of 92 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.460mg/ml (1.00mM)	Taking the 1 mL working solution as an example, add 50 μL of 9.2 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

Preparing Stock Solutions

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

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.

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