Paxalisib
Based on 5 publication(s) in Google Scholar
Paxalisib (GDC-0084) is a brain penetrant inhibitor of PI3K and mTOR, with Kis of 2 nM, 46 nM, 3 nM, 10 nM and 70 nM for PI3Kα PI3Kβ, PI3Kδ, PI3Kγ and mTOR, respectively.
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- 純度: 99.51%
- CAS 番号: 1382979-44-3
- 分子式: C18H22N8O2
- 分子量:382.42
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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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MedChemExpress（MCE）の使用を引用している文献 Paxalisib
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Customer Validation & Images
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Cell Proliferation/Viability Assay
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WB
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2D/3D Cell Culture and Differentiation
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IF
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WB
生物活性
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PI3Kα 2 nM (Ki) |
PI3Kδ 3 nM (Ki) |
PI3Kγ 10 nM (Ki) |
PI3Kβ 46 nM (Ki) |
mTOR 70 nM (Ki) |
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Cell Line
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Type | Value | Description | References |
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| PC-3 | EC50 |
0.4 μM
Compound: 16
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Antiproliferative activity against human PC3 cells after 3 days by CellTitre-Glo assay
Antiproliferative activity against human PC3 cells after 3 days by CellTitre-Glo assay
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[PMID: 27096040] |
| SF-268 | EC50 |
1.01 μM
Compound: 16
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Antiproliferative activity against human SF268 cells after 4 days by CellTitre-Glo assay
Antiproliferative activity against human SF268 cells after 4 days by CellTitre-Glo assay
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[PMID: 27096040] |
| U-87MG ATCC | EC50 |
0.74 μM
Compound: 16
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Antiproliferative activity against human U87 cells after 4 days by CellTitre-Glo assay
Antiproliferative activity against human U87 cells after 4 days by CellTitre-Glo assay
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[PMID: 27096040] |
Paxalisib (GDC-0084; Compound 16) maintains inhibition of each of the Class I PI3K isoforms but with more potent inhibition of mTOR. Paxalisib is also tested in five different GBM cell lines and is found to have antiproliferative EC50s ranging from 0.3 to 1.1 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| 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 1382979-44-3
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性状 Solid
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分子量 382.42
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分子式 C18H22N8O2
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Color White to off-white
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SMILES
NC1=NC=C(C2=NC(N3CCOCC3)=C4N=C(C(C)(C)OCC5)N5C4=N2)C=N1
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別名
GDC-0084
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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 (5)
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Journal Impact Factor
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Most Recent
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Autophagy
Activation of chaperone-mediated autophagy suppresses glioblastoma by promoting wild-type IDH1/isocitrate dehydrogenase 1 degradation. [Abstract]2025 Nov 30:1-21. PMID: 41231102
Paxalisib purchased from MedChemExpress. Usage Cited in: Autophagy. 2025 Nov 30:1-21. [Abstract]
Paxalisib (72 h) reduced the viability of both U251 and U87 cells with IC50 values of 1.551 μM and 1.371 μM, respectively.
Paxalisib purchased from MedChemExpress. Usage Cited in: Autophagy. 2025 Nov 30:1-21. [Abstract]
Paxalisib (1–2 μM; 24 h) reduced the expression levels of IDH1 and CCND1 in U251 and U87 cells.
Paxalisib purchased from MedChemExpress. Usage Cited in: Autophagy. 2025 Nov 30:1-21. [Abstract]
Representative bright-field microscopy images of patient-derived GSC#40 treated with DMSO (control), Paxalisib (2 μM), or metformin (10 mM) at days 1, 3, and 7 of culture. Scale bar: 400 mm. The results showed that Paxalisib (2 μM) significantly retarded the growth of cell spheroids throughout the seven-day observation period.
Paxalisib purchased from MedChemExpress. Usage Cited in: Autophagy. 2025 Nov 30:1-21. [Abstract]
Immunofluorescence analysis showing colocalization of IDH1 (red) and LAMP1 (green) in GSC#40 treated with DMSO (control), Paxalisib (2 μM), or metformin (10 mM) for 7 days. White arrows indicate co-localized puncta, indicating lysosomal trafficking of IDH1. DAPI (blue) was used for nuclei staining. Original magnification: 100x. Scale bar: 40 μm.
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Front Pharmacol
CC-223, NSC781406, and BGT226 Exerts a Cytotoxic Effect Against Pancreatic Cancer Cells via mTOR Signaling. [Abstract]2020 Nov 11;11:580407. PMID: 33343350 -
Biochem Biophys Res Commun
2018 Sep 10;503(3):1941-1948. PMID: 30072096
Paxalisib purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2018 Sep 10;503(3):1941-1948. [Abstract]
Paxalisib (GDC-0084, 100-1000 nM; 30 h) significantly upregulated the expression of cleaved-caspase-3 and cleaved-caspase-9 in treated A431 cells.
Paxalisib purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2018 Sep 10;503(3):1941-1948. [Abstract]
Paxalisib (GDC-0084, 100–1000 nM; 72 h) inhibited the survival of all cSCC cells.
Paxalisib purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2018 Sep 10;503(3):1941-1948. [Abstract]
Paxalisib (GDC-0084, 10-1000 nM; 30 h) treatment in A431 cells dose-dependently increased the activities of caspase-3 and caspase-9.
Paxalisib purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2018 Sep 10;503(3):1941-1948. [Abstract]
Paxalisib (GDC-0084, 10-1000 nM; 48 h) dose-dependently increased histone-bound DNA ELISA OD in A431 cells.
Paxalisib purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2018 Sep 10;503(3):1941-1948. [Abstract]
Paxalisib (GDC-0084, 500 nM; 48 h) induced apoptosis activation in A431 cells.
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溶剤 & 溶解度
DMSO : 7.69 mg/mL (20.11 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, 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)
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: 1 mg/mL (2.61 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 1 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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: 1 mg/mL (2.61 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 1 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: 0.5% Methylcellulose/0.2% Tween-80 in Saline water
Solubility: 4.99 mg/mL (13.05 mM); Suspended solution; Need ultrasonic
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.
プロトコル
Mice[1]
PTEN-null U-87 MG/M human glioblastoma cancer cells are cultured in RPMI 1640 media plus 1% L-glutamine with 10% fetal bovine serum. Cells in log-phase growth are harvested and resuspended in HBSS:Matrigel (1:1, v:v) for injection into female NCr nude mice aged 20 weeks. Animals receive five million cells subcutaneously in the right lateral thorax in 0.1 mL. Mice bearing established tumors in the range of 200-500 mm3 are separated into groups of equally sized tumors (n=6-7/group) to receive escalating doses of Paxalisib. Paxalisib is formulated once weekly in 0.5% methylcellulose and 0.2% Tween-80 at concentrations needed for target doses in a volume of 0.2 mL. All formulations are stored in a refrigerator and brought to room temperature and mixed well by vortex before oral administration by gavage once daily for 23 days. Tumor volumes are calculated. Changes in body weights are reported as a percentage change from the starting weight.
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
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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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6149 mL | 13.0746 mL | 26.1493 mL | 65.3731 mL |
| 5 mM | 0.5230 mL | 2.6149 mL | 5.2299 mL | 13.0746 mL | |
| 10 mM | 0.2615 mL | 1.3075 mL | 2.6149 mL | 6.5373 mL | |
| 15 mM | 0.1743 mL | 0.8716 mL | 1.7433 mL | 4.3582 mL | |
| 20 mM | 0.1307 mL | 0.6537 mL | 1.3075 mL | 3.2687 mL |
Paxalisib 関連分類
HY-19962 関連分類
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