| Field | Specification |
|---|---|
| Target | |
| Alternative names | GDC-0032; RG-7604 |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C24H28N8O2 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
Taselisib, also known as GDC-0032 or RG-7604, is a potent PI3K inhibitor that targets PIK3CA mutations, with Ki values of 0.12 nM, 0.29 nM, 0.97 nM and 9.1 nM against PI3Kδ, PI3Kα, PI3Kγ and PI3Kβ, respectively. It is supplied as a white to off-white solid (C24H28N8O2, MW 460.53) at 99.75% purity.
Physical & Chemical Properties
| CAS Number | 1282512-48-4 |
|---|---|
| Molecular Formula | C24H28N8O2 |
| Molecular Weight | 460.53 g/mol |
| Purity | 99.75% |
| Appearance | Solid |
| Color | White to off-white |
| 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 |
| Target | PI3Kδ, PI3Kα, PI3Kγ, PI3Kβ |
| Signaling Pathway | PI3K/Akt/mTOR |
| Solubility | In Vitro: DMSO: 25 mg/mL (54.29 mM; Requires sonication and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 1 year; -20°C, 6 months. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target[3]
|
PI3Kδ 0.12 nM (Ki) |
PI3Kα 0.29 nM (Ki) |
PI3Kγ 0.97 nM (Ki) |
PI3Kβ 9.1 nM (Ki) |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 25 mg/mL (54.29 mM) | requires sonication and warming and heat to 60°C; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 1 year) or -20°C (up to 6 months); avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 2.5 mg/mL (5.43 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | ≥ 2.5 mg/mL (5.43 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Protocol 3
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 2.5 mg/mL (5.43 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL corn oil. |
Data provided by the manufacturer.
In Vitro
In PIK3CA mutant cell lines, AKT/mTOR signaling is inhibited by Taselisib (GDC-0032) (100 nM), but cells with loss or mutation of PTEN are not affected in this way. In head and neck cancer cell lines sensitive to its single-agent activity, Taselisib (GDC-0032) enhances radiation-induced apoptosis and inhibits growth[1]. The effects of MEK1/2 inhibition are enhanced by Taselisib (GDC-0032) in BRAFV600E/PTENNull human melanoma cells and in autochthonous mouse melanomas[2].
In Vivo
Taselisib (GDC-0032) (5 mg/kg, p.o.) potently impairs PI3K signaling and boosts the efficacy of fractionated radiotherapy. In nude mice implanted with subcutaneous Cal-33 xenografts, Taselisib (GDC-0032) combined with radiation is more effective than either treatment alone[1]. After treatment with Taselisib (GDC-0032) (22.5 mg/kg, p.o.), vehicle-treated BRAFV600E/PTENNull melanoma-bearing mice show initial tumor regression[2].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
Cell Assay[1]
Seed cells in replicates of 6 in 96-well plates at 500 to 5,000 cells/well overnight, then treat with Taselisib (GDC-0032). After 4 days, remove the media and fix the cells with 4% glutaraldehyde for 30 minutes. Stain the fixed cells with 0.1% crystal violet for 2 minutes, wash, and dissolve in 10% acetic acid.
Animal Administration[1]
Inject 5×105 cells bilaterally into six-week-old Nu/Nu mice, with the cells resuspended in 200 μL of culture media and Matrigel mixed 1:1. After tumors reach approximately 100 to 200 cm3, randomize mice into treatment arms with 8 to 10 tumors per group. Dissolve Taselisib (GDC-0032) (5 mg/kg) in a vehicle containing 0.5% methylcellulose with 0.2% TWEEN-80 and administer it by daily oral gavage.
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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Suppression of insulin feedback enhances the efficacy of PI3K inhibitors. Nature 2018 Aug;560(7719):499-503. PMID: 30051890
Microbiome metabolism of dietary phytochemicals controls the anticancer activity of PI3K inhibitors. Cell 2025 May 29;188(11):3065-3080.e21. PMID: 40393457
A first-in-class selective inhibitor of EGFR and PI3K offers a single-molecule approach to targeting adaptive resistance. Nat Cancer 2024 Aug;5(8):1250-1266. PMID: 38992135
Genomic Alterations in PIK3CA-Mutated Breast Cancer Result in mTORC1 Activation and Limit the Sensitivity to PI3Kα Inhibitors. Cancer Res 2021 May 1;81(9):2470-2480. PMID: 33685991
NTRK2 activation cooperates with PTEN deficiency in T-ALL through activation of both the PI3K-AKT and JAK-STAT3 pathways. Cell Discov 2016 Sep 20:2:16030. PMID: 27672444
WWP1 inactivation enhances efficacy of PI3K inhibitors while suppressing their toxicities in breast cancer models. J Clin Invest 2021 Dec 15;131(24):e140436. PMID: 34907909
Fibroblast growth factor 18 exerts anti-osteoarthritic effects through PI3K-AKT signaling and mitochondrial fusion and fission. Pharmacol Res 2019 Jan:139:314-324. PMID: 30273654
Surface roughness-induced absorption acts as an ovarian cancer cells growth sensor-monitor. Biosens Bioelectron 2020 Aug 1:161:112240.
Fibrinogen/AKT/Microfilament Axis Promotes Colitis by Enhancing Vascular Permeability. Cell Mol Gastroenterol Hepatol 2021;11(3):683-696. PMID: 33075564
Dual CCNE1/PIK3CA targeting is synergistic in CCNE1-amplified/PIK3CA-mutated uterine serous carcinomas in vitro and in vivo. Br J Cancer 2016 Jul 26;115(3):303-11.
