Taselisib
Based on 23 publication(s) in Google Scholar
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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.75%
- No. CAS: 1282512-48-4
- Fòrmula: C24H28N8O2
- Peso molecular:460.53
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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DactolisibPI3K/mTOR Inhibitor
Publications Citing Use of MedChemExpress (MCE) Taselisib
More- Nature. 2018 Aug;560(7719):499-503. [Abstract]
- Cell. 2025 May 29;188(11):3065-3080.e21. [Abstract]
- Nat Cancer. 2024 Aug;5(8):1250-1266. [Abstract]
- Cancer Res. 2021 May 1;81(9):2470-2480. [Abstract]
- Cell Discov. 2016 Sep 20:2:16030. [Abstract]
- J Clin Invest. 2021 Dec 15;131(24):e140436. [Abstract]
- Pharmacol Res. 2019 Jan:139:314-324. [Abstract]
- Biosens Bioelectron. 2020 Aug 1:161:112240. [Abstract]
- Cell Mol Gastroenterol Hepatol. 2021;11(3):683-696. [Abstract]
- Br J Cancer. 2016 Jul 26;115(3):303-11. [Abstract]
- Cell Rep. 2024 Apr 23;43(5):114132. [Abstract]
- Mol Cancer Ther. 2015 Nov;14(11):2519-26. [Abstract]
- Oncol Rep. 2018 Dec;40(6):3469-3478. [Abstract]
- BMC Genomics. 2018 Dec 6;19(1):881. [Abstract]
- Pathol Res Pract. 2026 Jun:282:156475. [Abstract]
- bioRxiv. 2026 Jul 3.
- bioRxiv. 2025 Oct 25.
- bioRxiv. 2024 Nov 6:2024.11.04.621884. [Abstract]
- Patent. US20210236501A1.
- Universidad de Las Palmas de Gran Canaria. 2023 May 24.
- Patent. US20220249511A1.
- Oxid Med Cell Longev. 2020 Nov 26:2020:3648040. [Abstract]
- Methods Mol Biol. 2018:1711:351-398. [Abstract]
Customer Validation & Images
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In Vivo Efficacy Study
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Bio/Physico-chemical Assay
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Bio/Physico-chemical Assay
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Cell Imaging/Staining
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Cell Imaging/Staining
Actividad biológica
Descripciòn
IC50 & Target
[3]|
PI3Kδ 0.12 nM (Ki) |
PI3Kα 0.29 nM (Ki) |
PI3Kγ 0.97 nM (Ki) |
PI3Kβ 9.1 nM (Ki) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| PC-3 | EC50 |
0.571 μM
Compound: 11l, GDC-0032
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Cytotoxicity against human PC3 cells
Cytotoxicity against human PC3 cells
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[PMID: 23662903] |
| PC-3 | IC50 |
0.031 μM
Compound: 11l, GDC-0032
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Inhibition of PI3Kalpha in human PC3 cells assessed as reduction of AKT phosphorylation
Inhibition of PI3Kalpha in human PC3 cells assessed as reduction of AKT phosphorylation
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[PMID: 23662903] |
In Vitro
Taselisib (GDC-0032) (100 nM) inhibits AKT/mTOR signaling in PIK3CA mutant cell lines but not in cells with loss or mutation of PTEN; Taselisib (GDC-0032) enhances radiation-induced apoptosis and inhibits growth in head and neck cancer cell lines that are sensitive to its single-agent activiy[1]. Taselisib (GDC-0032) enhances the effects of MEK1/2 inhibition on both BRAFV600E/PTENNull human melanoma cells autochthonous mouse melanomas[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1282512-48-4
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Appearance Solid
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Peso molecular 460.53
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Fòrmula C24H28N8O2
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Color White to off-white
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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
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Synonyms
GDC-0032; RG-7604
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (23)
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Journal Impact Factor
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Most Recent
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Nature
2018 Aug;560(7719):499-503. PMID: 30051890
Taselisib purchased from MedChemExpress. Usage Cited in: Nature. 2018 Aug;560(7719):499-503. [Abstract]
Mean with standard deviation of c-Peptide levels assessed at 240 min (p-values comparing vehicle treatment to BKM120, BYL-719, and GDC-0032 (Taselisib, 25 mg/kg) by two sided t-test were 0.017, <0.0001, and 0.007 respectively).
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Cell
Microbiome metabolism of dietary phytochemicals controls the anticancer activity of PI3K inhibitors. [Abstract]2025 May 29;188(11):3065-3080.e21. PMID: 40393457 -
Nat Cancer
A first-in-class selective inhibitor of EGFR and PI3K offers a single-molecule approach to targeting adaptive resistance. [Abstract]2024 Aug;5(8):1250-1266. PMID: 38992135
Taselisib purchased from MedChemExpress. Usage Cited in: Nat Cancer. 2024 Aug;5(8):1250-1266. [Abstract]
Blood glucose levels in mice treated with a panel of PI3K inhibitors (n = 8 mice per group for vehicle, MTX-531, alpelisib or buparlisib; n = 5 mice per group for copanlisib and taselisib (25 mg/kg); n = 3 mice per group for omipalisib).
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Cancer Res
Genomic Alterations in PIK3CA-Mutated Breast Cancer Result in mTORC1 Activation and Limit the Sensitivity to PI3Kα Inhibitors. [Abstract]2021 May 1;81(9):2470-2480. PMID: 33685991
Taselisib purchased from MedChemExpress. Usage Cited in: Cancer Res. 2021 May 1;81(9):2470-2480. [Abstract]
Plot of the candidate genes from CRISPR-Cas9 KO screen in MCF7 cells treated with 60 nM taselisib. Top candidate genes are highlighted in the indicated colors.
Taselisib purchased from MedChemExpress. Usage Cited in: Cancer Res. 2021 May 1;81(9):2470-2480. [Abstract]
We observed that loss of the shared candidates, the TSC1/TSC2 complex, the GATOR1 complex and the positive control PTEN, had the most dramatic effects on limiting the sensitivity to alpelisib and taselisib in both MCF7 and T47D cells.
Taselisib purchased from MedChemExpress. Usage Cited in: Cancer Res. 2021 May 1;81(9):2470-2480. [Abstract]
WT and DEPDC5 KO MCF7 and T47D cells stably expressing the indicated constructs were treated with DMSO, 1 μM alpelisib, 60 nM taselisib, 2 μM GDC0068 or 20 nM everolimus for 6 days and stained with crystal violet.
Taselisib purchased from MedChemExpress. Usage Cited in: Cancer Res. 2021 May 1;81(9):2470-2480. [Abstract]
T47D cells expressing different forms of RagA were treated with DMSO, 1 μM alpelisib, 60 nM taselisib, 2 μM GDC0068, 2 μM MK2206 or 20 nM everolimus for 6 days and stained with crystal violet.
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Cell Discov
NTRK2 activation cooperates with PTEN deficiency in T-ALL through activation of both the PI3K-AKT and JAK-STAT3 pathways. [Abstract]2016 Sep 20:2:16030. PMID: 27672444
Taselisib purchased from MedChemExpress. Usage Cited in: Cell Discov. 2016 Sep 20:2:16030. [Abstract]
Effects of combined inhibition of PI3K and STAT3 pathways on PTEN-mutated T-ALL cells. (a) Short-term treatment of Ba/F3-shPTEN-NTRK2-Tel cells with isoform-selective inhibitors and Pan-PI3K inhibitor GDC-0032. Cells are treated with DMSO, BYL719, KIN193, GS-1101, GDC-0032 (1 μM) or JAK–STAT inhibitor AZD-1480 (1 μM) for 3 h (n=3) for each treatment. (b) Immunoblot analysis of P-Akt and p-S6 in PF382 and JURKAT cells. Cells are treated with the same inhibitors as in a. (c) Combination of siNTRK2
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J Clin Invest
WWP1 inactivation enhances efficacy of PI3K inhibitors while suppressing their toxicities in breast cancer models. [Abstract]2021 Dec 15;131(24):e140436. PMID: 34907909 -
Pharmacol Res
Fibroblast growth factor 18 exerts anti-osteoarthritic effects through PI3K-AKT signaling and mitochondrial fusion and fission. [Abstract]2019 Jan:139:314-324. PMID: 30273654 -
Biosens Bioelectron
Surface roughness-induced absorption acts as an ovarian cancer cells growth sensor-monitor. [Abstract]2020 Aug 1:161:112240. PMID: 32365013 -
Cell Mol Gastroenterol Hepatol
2021;11(3):683-696. PMID: 33075564 -
Br J Cancer
Dual CCNE1/PIK3CA targeting is synergistic in CCNE1-amplified/PIK3CA-mutated uterine serous carcinomas in vitro and in vivo. [Abstract]2016 Jul 26;115(3):303-11. PMID: 27351214
Taselisib purchased from MedChemExpress. Usage Cited in: Br J Cancer. 2016 Jul 26;115(3):303-11. [Abstract]
Effect of the combination of CYC065 and Taselisib in vitro. (A) Uterine serous carcinoma-ARK-1 and USC-ARK-2 are treated with the half-maximal inhibitory concentration (IC50) of CYC065, the IC50 of Taselisib (GDC0032) or the combination of the IC50s of the two compounds for 72 h. Cell counting is then carried. The incubation of USC-ARK-1 and USC-ARK-2 cells with the combination of CYC065 and Taselisib is significantly more effective in inhibiting cells’ growth th
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Cell Rep
Adipocyte PI3K links adipostasis with baseline insulin secretion at fasting through an adipoincretin effect. [Abstract]2024 Apr 23;43(5):114132. PMID: 38656871 -
Mol Cancer Ther
Dual HER2/PIK3CA Targeting Overcomes Single-Agent Acquired Resistance in HER2-Amplified Uterine Serous Carcinoma Cell Lines In Vitro and In Vivo. [Abstract]2015 Nov;14(11):2519-26. PMID: 26333383 -
Oncol Rep
MicroRNA‑433 inhibits cell growth and induces apoptosis in human cervical cancer through PI3K/AKT signaling by targeting FAK. [Abstract]2018 Dec;40(6):3469-3478. PMID: 30272334 -
BMC Genomics
Proto-oncogenes in a eukaryotic unicellular organism play essential roles in plasmodial growth in host cells. [Abstract]2018 Dec 6;19(1):881. PMID: 30522435 -
Pathol Res Pract
Identification of bioactive components in Wuji Wan and their protective effects against gastric ulcer via regulating PIK3CA-mediated PI3K/AKT pathway. [Abstract]2026 Jun:282:156475. PMID: 42001845 -
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bioRxiv
PAIRWISE: Deep Learning-based Prediction of Effective Personalized Drug Combinations in Cancer. [Abstract]2024 Nov 6:2024.11.04.621884. PMID: 39574568 -
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Oxid Med Cell Longev
Metformin Prevents Follicular Atresia in Aging Laying Chickens through Activation of PI3K/AKT and Calcium Signaling Pathways. [Abstract]2020 Nov 26:2020:3648040. PMID: 33294120 -
Methods Mol Biol
2018:1711:351-398. PMID: 29344898
Solvente y solubilidad
In Vitro:
DMSO : 25 mg/mL (54.29 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.43 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.43 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocolo
Cell Assay[1]
Cells are seeded in replicates of 6 in 96-well plates with 500 to 5,000 cells/well overnight and then treated with Taselisib (GDC-0032). After 4 days, the media are removed and the cells are fixed with 4% glutaraldehyde for 30 minutes. Fixed cells are stained with 0.1% crystal violet for 2 minutes, then washed, and dissolved in 10% acetic acid.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration[1]
Six-week-old Nu/Nu mice are injected bilaterally with 5×105 cells resuspended in 200 μL of culture media and Matrigel mixed in a 1:1 ratio. After tumors reache approximately 100 to 200 cm3, mice are randomized into treatment arms with 8 to 10 tumors per group. Taselisib (GDC-0032) (5 mg/kg) is dissolved in a vehicle containing 0.5% methylcellulose with 0.2% TWEEN-80 and is administered via daily oral gavage.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (284 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.1714 mL | 10.8571 mL | 21.7141 mL | 54.2853 mL |
| 5 mM | 0.4343 mL | 2.1714 mL | 4.3428 mL | 10.8571 mL | |
| 10 mM | 0.2171 mL | 1.0857 mL | 2.1714 mL | 5.4285 mL | |
| 15 mM | 0.1448 mL | 0.7238 mL | 1.4476 mL | 3.6190 mL | |
| 20 mM | 0.1086 mL | 0.5429 mL | 1.0857 mL | 2.7143 mL | |
| 25 mM | 0.0869 mL | 0.4343 mL | 0.8686 mL | 2.1714 mL | |
| 30 mM | 0.0724 mL | 0.3619 mL | 0.7238 mL | 1.8095 mL | |
| 40 mM | 0.0543 mL | 0.2714 mL | 0.5429 mL | 1.3571 mL | |
| 50 mM | 0.0434 mL | 0.2171 mL | 0.4343 mL | 1.0857 mL |
Taselisib Related Classifications
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