製品番号: HY-13898

Taselisib

(別名: GDC-0032; RG-7604)

21 Cited Publications

カスタマーレビュー

Based on 21 publication(s) in Google Scholar

Taselisib (GDC-0032) is a potent PI3K inhibitor targets PIK3CA mutations, with K_is of 0.12 nM, 0.29 nM, 0.97 nM, and 9.1 nM for PI3Kδ, PI3Kα, PI3Kγ and PI3Kβ, respectively.

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研究用途以外に使用した場合、当社は一切の責任を負いかねます。

純度: 99.75%
CAS 番号: 1282512-48-4
分子式: C₂₄H₂₈N₈O₂
分子量:460.53

保管条件:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

Taselisib 構造式

CAS 番号: 1282512-48-4

容量

価格（税別）

在庫状況

数量

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- 体内実験
- 臨床実験
化学情報
Publications (21)
溶剤 & 溶解度
- 体外
- 体内
プロトコル
純度とドキュメンテーション
参考文献
Help & FAQs
関連分類
Bioz

生物活性

製品説明

Taselisib (GDC-0032) is a potent PI3K inhibitor targets PIK3CA mutations, with K_is of 0.12 nM, 0.29 nM, 0.97 nM, and 9.1 nM for PI3Kδ, PI3Kα, PI3Kγ and PI3Kβ, respectively.

IC₅₀ & Target^[3]

PI3Kδ

0.12 nM (Ki)

PI3Kα

0.29 nM (Ki)

PI3Kγ

0.97 nM (Ki)

PI3Kβ

9.1 nM (Ki)

PI3K アイソフォーム固有の製品をすべて表示 :

Cellular Effect

Cell Line	Type	Value	Description	References
PC-3	EC₅₀	0.571 μM Compound: 11l, GDC-0032	Cytotoxicity against human PC3 cells Cytotoxicity against human PC3 cells	[PMID: 23662903]
PC-3	IC₅₀	0.031 μM Compound: 11l, GDC-0032	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	[PMID: 23662903]

体外実験

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 BRAF^V600E/PTEN^Null human melanoma cells autochthonous mouse melanomas^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

体内実験

Taselisib (GDC-0032) (5 mg/kg, p.o.) potently impairs PI3K signaling and enhances the efficacy of fractionated radiotherapy; Taselisib (GDC-0032) and radiation is more effective than either treatment alone in nude mice implanted with subcutaneous Cal-33 xenografts^[1]. The vehicle-treated BRAFV600E/PTENNull melanoma-bearing mice experiencs initial tumor regression after treatment with Taselisib (GDC-0032) (22.5 mg/kg, p.o.)^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

臨床実験

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

化学情報

CAS 番号 1282512-48-4
性状 Solid
分子量 460.53
分子式 C₂₄H₂₈N₈O₂
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
別名

GDC-0032; RG-7604
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (21)

All In Vivo Efficacy StudyBio/Physico-chemical AssayCell Imaging/StainingWB

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Journal Impact Factor

Nature

Suppression of insulin feedback enhances the efficacy of PI3K inhibitors. [Abstract]

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).
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).
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.
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
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
Biosens Bioelectron

Surface roughness-induced absorption acts as an ovarian cancer cells growth sensor-monitor. [Abstract]

2020 Aug 1;161:112240. PMID: 32365013
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
Cell Mol Gastroenterol Hepatol

Fibrinogen/AKT/Microfilament Axis Promotes Colitis by Enhancing Vascular Permeability. [Abstract]

2021;11(3):683-696. PMID: 33075564
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
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
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
bioRxiv

2025 Oct 25.
bioRxiv

PAIRWISE: Deep Learning-based Prediction of Effective Personalized Drug Combinations in Cancer. [Abstract]

2024 Nov 6:2024.11.04.621884. PMID: 39574568
Patent

US20210236501A1.
Universidad de Las Palmas de Gran Canaria

2023 May 24.
Patent

US20220249511A1.
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

Methods for High-throughput Drug Combination Screening and Synergy Scoring. [Abstract]

2018:1711:351-398. PMID: 29344898

溶剤 & 溶解度

体外:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.1714 mL

10.8571 mL

21.7141 mL

5 mM

0.4343 mL

2.1714 mL

4.3428 mL

10 mM

0.2171 mL

1.0857 mL

2.1714 mL

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.

モル濃度計算機

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.43 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

プロトコル

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.

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

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元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
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IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
取扱説明書 (2659 KB)

参考文献

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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
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

Keywords

Taselisib

21 Cited Publications

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Taselisib

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MedChemExpress（MCE）の使用を引用している文献 Taselisib

PI3K アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (21)

溶剤 & 溶解度

プロトコル

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

Taselisib 関連分類

製品番号: HY-13898