Art. -Nr.: HY-19962

Paxalisib

(Synonyms: GDC-0084)

5 Cited Publications

Kundenbewertung

Based on 5 publication(s) in Google Scholar

Paxalisib (GDC-0084) is a brain penetrant inhibitor of PI3K and mTOR, with K_is of 2 nM, 46 nM, 3 nM, 10 nM and 70 nM for PI3Kα PI3Kβ, PI3Kδ, PI3Kγ and mTOR, respectively.

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Reinheit: 99.51%
CAS. Nr.: 1382979-44-3
Formel: C₁₈H₂₂N₈O₂
Molecular Weight:382.42

Speicherung:

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

Paxalisib Chemical Structure

CAS. Nr.: 1382979-44-3

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Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (5)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Paxalisib (GDC-0084) is a brain penetrant inhibitor of PI3K and mTOR, with K_is of 2 nM, 46 nM, 3 nM, 10 nM and 70 nM for PI3Kα PI3Kβ, PI3Kδ, PI3Kγ and mTOR, respectively^[1].

IC₅₀ & Target^[1]

PI3Kα

2 nM (Ki)

PI3Kδ

3 nM (Ki)

PI3Kγ

10 nM (Ki)

PI3Kβ

46 nM (Ki)

mTOR

70 nM (Ki)

Alle PI3K Isoform-spezifische Produkte anzeigen :

Alle mTOR Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
PC-3	EC₅₀	0.4 μM Compound: 16	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	[PMID: 27096040]
SF-268	EC₅₀	1.01 μM Compound: 16	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	[PMID: 27096040]
U-87MG ATCC	EC₅₀	0.74 μM Compound: 16	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	[PMID: 27096040]

In Vitro

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.

In Vivo

After a 25 mg/kg dose of Paxalisib (GDC-0084; Compound 16) administered orally, pAKT in normal mouse brain tissue is significantly inhibited at 1 and 6 h postdose. The potent inhibition of pAKT at both time points in this study demonstrates that Paxalisib inhibits its target behind a fully intact BBB. In addition to the pharmacodynamic effect in normal brain tissue, Paxalisib is studied in a subcutaneous U87 tumor xenograft model of glioblastoma in mice. In this study, Paxalisib achieves significant and dose-dependent tumor growth inhibition. Tumor growth inhibition is first observed at a 2.2 mg/kg dose level. Higher doses led to greater tumor growth inhibition, including tumor regressions at the 17.9 mg/kg dose level. Each of these doses is well tolerated for the duration of the study^[1].

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

Clinical Trial

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

Chemical Information

CAS. Nr. 1382979-44-3
Appearance Solid
Molecular Weight 382.42
Formel C₁₈H₂₂N₈O₂
Color White to off-white
SMILES

NC1=NC=C(C2=NC(N3CCOCC3)=C4N=C(C(C)(C)OCC5)N5C4=N2)C=N1
Synonyms

GDC-0084
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Publications (5)

All WB2D/3D Cell Culture and DifferentiationIFCell Proliferation/Viability AssayApoptosis AnalysisELISAFlow Cytometry

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Journal Impact Factor

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.
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

GDC-0084 inhibits cutaneous squamous cell carcinoma cell growth. [Abstract]

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.
bioRxiv

2025 Dec 5.
Res Sq

2025 Apr 14.

Lösungsmittel & Löslichkeit

In Vitro:

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)

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

2.6149 mL

13.0746 mL

26.1493 mL

5 mM

0.5230 mL

2.6149 mL

5.2299 mL

10 mM

0.2615 mL

1.3075 mL

2.6149 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, 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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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: 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.

Protocol 2

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.

Protocol 3

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

Solubility: ≥ 1 mg/mL (2.61 mM); Clear solution

This protocol yields a clear solution of ≥ 1 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 (10.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

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.

Protocol 1

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

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

Protokoll

Animal Administration^[1]

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.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (284 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Heffron TP, et al. Discovery of Clinical Development Candidate GDC-0084, a Brain Penetrant Inhibitor of PI3K and mTOR. ACS Med Chem Lett. 2016 Feb 16;7(4):351-6. [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, 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

Keywords

Paxalisib

5 Cited Publications

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Paxalisib

Kinase Inhibitor Library

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Posttranslational Modification Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) Paxalisib

Alle PI3K Isoform-spezifische Produkte anzeigen

Alle mTOR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (5)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Paxalisib Related Classifications

HY-19962 Related Classifications