Inavolisib
Based on 11 publication(s) in Google Scholar
Inavolisib (GDC-0077) is a potent, orally active, and selective PI3Kα inhibitor (IC50=0.038 nM). Inavolisib exerts its activity by binding to the ATP binding site of PI3K, thereby inhibiting the phosphorylation of PIP2 to PIP3. Inavolisib is more selective for mutant versus wild-type PI3Kα. Inavolisib can be used for the study of breast cancer.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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 : 99.96%
- CAS 番号: 2060571-02-8
- 分子式: C18H19F2N5O4
- 分子量:407.37
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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生物活性
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化学情報
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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
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Help & FAQs
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MedChemExpress（MCE）の使用を引用している文献 Inavolisib
More- Int J Biol Sci. 2025 Mar 19;21(6):2462-2475. [Abstract]
- Clin Transl Med. 2022 May;12(5):e835. [Abstract]
- Cancer Metab. 2025 Feb 7;13(1):6. [Abstract]
- Int J Mol Sci. 2024 Jun 1;25(11):6111. [Abstract]
- Cancer Sci. 2023 Jul;114(7):2951-2960. [Abstract]
- Neoplasia. 2026 Jun:76:101305. [Abstract]
- Cell Signal. 2026 Mar:139:112351. [Abstract]
- In Vivo. 2026 Sep-Oct;40(5):2663-2669.
- bioRxiv. 2026 Sep 22:2026.09.21.753236.
- Harvard University. 2026.
- medRxiv. 2026 Jan 23:2026.01.21.26344562. [Abstract]
Customer Validation & Images
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Cell Proliferation/Viability Assay
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Cell Proliferation/Viability Assay
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WB
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WB
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Cell Proliferation/Viability Assay
生物活性
製品説明
IC50 & Target
[1]|
PI3Kα 0.038 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCC1954 | EC50 |
60 nM
Compound: 32; GDC-0077
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Antiproliferative activity against human HCC1954 cells assessed as reduction in cell viability incubated for 4 days by Celltiter-Glo luminescence assay
Antiproliferative activity against human HCC1954 cells assessed as reduction in cell viability incubated for 4 days by Celltiter-Glo luminescence assay
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[PMID: 36455032] |
| MCF7 | EC50 |
30 nM
Compound: 32; GDC-0077
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Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 4 days by Celltiter-Glo luminescence assay
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 4 days by Celltiter-Glo luminescence assay
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[PMID: 36455032] |
体外実験
Inavolisib (GDC-0077) is >300-fold more selective for PI3Kα over the other class I PI3K isoforms (β, δ, and γ) and >2000-fold more selective over PIK family members. Inavolisib selectively degrades mutant PI3Kα in a proteasome-dependent fashion resulting in reduction of PI3K pathway activity biomarkers such as pAKT and pPRAS40, inhibition of cell proliferation, and increased apoptosis in human PIK3CA-mutant breast cancer cell lines to a greater extent when compared to PIK3CA wild-type cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
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
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 2060571-02-8
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性状 Solid
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分子量 407.37
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分子式 C18H19F2N5O4
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Color White to yellow
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SMILES
C[C@@H](C(N)=O)NC1=CC=C(C2=NC(N3[C@H](C(F)F)COC3=O)=CN2CCO4)C4=C1
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別名
GDC-0077; RG6114
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (11)
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Journal Impact Factor
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Most Recent
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Int J Biol Sci
The SGK3/GSK3β/β-catenin signaling promotes breast cancer stemness and confers resistance to alpelisib therapy. [Abstract]2025 Mar 19;21(6):2462-2475. PMID: 40303291
Inavolisib purchased from MedChemExpress. Usage Cited in: Int J Biol Sci. 2025 Mar 19;21(6):2462-2475. [Abstract]
Dose-response curves for Inavolisib (0.1-100 μM ) in parental and alpelisib-resistant breast cancer cell lines.
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Clin Transl Med
Genome-wide gain-of-function screening identifies EZH2 mediating resistance to PI3Kα inhibitors in oesophageal squamous cell carcinoma. [Abstract]2022 May;12(5):e835. PMID: 35604910
Inavolisib purchased from MedChemExpress. Usage Cited in: Clin Transl Med. 2022 May;12(5):e835. [Abstract]
EZH2 overexpression was conferred in esophageal squamous cell carcinoma (ESCC) cells. EV32 and HE6 cells were treated with GDC-0077 (0.1-10 μM) for 72 hours, and cell proliferation was detected by SRB assay.
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Cancer Metab
CD36 inhibition enhances the anti-proliferative effects of PI3K inhibitors in PTEN-loss anti-HER2 resistant breast cancer cells. [Abstract]2025 Feb 7;13(1):6. PMID: 39920872
Inavolisib purchased from MedChemExpress. Usage Cited in: Cancer Metab. 2025 Feb 7;13(1):6. [Abstract]
The effects of Inavolisib (0-1.1 μM, 72 h) on the proliferation of SK-BR-3 and HCC1569 cells.
Inavolisib purchased from MedChemExpress. Usage Cited in: Cancer Metab. 2025 Feb 7;13(1):6. [Abstract]
The modulated protein levels of SCD-1 and CD36 were assessed by western blotting in SK-BR-3 cells treated with Inavolisib (0.5 μM) for 24 h.
Inavolisib purchased from MedChemExpress. Usage Cited in: Cancer Metab. 2025 Feb 7;13(1):6. [Abstract]
The modulated protein levels of SCD-1 and CD36 were assessed by western blotting in HCC1569 cells treated with Inavolisib (2 μM) for 24 h.
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Int J Mol Sci
2024 Jun 1;25(11):6111. PMID: 38892296 -
Cancer Sci
D-1553: A novel KRASG12C inhibitor with potent and selective cellular and in vivo antitumor activity. [Abstract]2023 Jul;114(7):2951-2960. PMID: 37158138 -
Neoplasia
PIK3CA mutant cervical cancer is selectively suppressed by PI3Kα inhibition (Alpelisib/BYL-719 and Inavolisib/GDC-0077) and cooperates with HPV directed T cell therapy. [Abstract]2026 Jun:76:101305. PMID: 41980433 -
Cell Signal
Nuclear SIRT6 depletion activates LINE1-cGAS-STING pathway to induce PASMCs senescence in hypoxic pulmonary hypertension. [Abstract]2026 Mar:139:112351. PMID: 41490817 -
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medRxiv
A Three-subtype Molecular model of Cervical Cancer: Multiple PI3K Pathway inhibitors suppress growth and cooperate with HPV-directed immunotherapy. [Abstract]2026 Jan 23:2026.01.21.26344562. PMID: 41646800
溶剤 & 溶解度
体外:
DMSO : 100 mg/mL (245.48 mM; Need ultrasonic; 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
体内:
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: ≥ 2.08 mg/mL (5.11 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (5.11 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Add each solvent one by one: 1% DMSO 99% Saline
Solubility: ≥ 0.55 mg/mL (1.35 mM); Clear solution
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.
純度とドキュメンテーション
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データシート (277 KB)
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SDS (644 KB)
- English - EN (644 KB)
- Français - FR (644 KB)
- Deutsch - DE (644 KB)
- Norwegian - NO (644 KB)
- Español - ES (644 KB)
- Swedish - SV (644 KB)
- Italian - IT (644 KB)
- Korean - KR (644 KB)
- Portuguese - PT (644 KB)
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取扱説明書 (2659 KB)
参考文献
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.4548 mL | 12.2739 mL | 24.5477 mL | 61.3693 mL |
| 5 mM | 0.4910 mL | 2.4548 mL | 4.9095 mL | 12.2739 mL | |
| 10 mM | 0.2455 mL | 1.2274 mL | 2.4548 mL | 6.1369 mL | |
| 15 mM | 0.1637 mL | 0.8183 mL | 1.6365 mL | 4.0913 mL | |
| 20 mM | 0.1227 mL | 0.6137 mL | 1.2274 mL | 3.0685 mL | |
| 25 mM | 0.0982 mL | 0.4910 mL | 0.9819 mL | 2.4548 mL | |
| 30 mM | 0.0818 mL | 0.4091 mL | 0.8183 mL | 2.0456 mL | |
| 40 mM | 0.0614 mL | 0.3068 mL | 0.6137 mL | 1.5342 mL | |
| 50 mM | 0.0491 mL | 0.2455 mL | 0.4910 mL | 1.2274 mL | |
| 60 mM | 0.0409 mL | 0.2046 mL | 0.4091 mL | 1.0228 mL | |
| 80 mM | 0.0307 mL | 0.1534 mL | 0.3068 mL | 0.7671 mL | |
| 100 mM | 0.0245 mL | 0.1227 mL | 0.2455 mL | 0.6137 mL |
Inavolisib 関連分類
HY-101562 関連分類
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