Name: Paxalisib (GDC-0084)
Brand: Selleck Chemicals
SKU: S8163
Availability: InStock
Rating: 5 (7 reviews)

Jump to

Quality Control

Batch: Purity: 99.02%

99.02

Related Targets	Akt mTOR GSK-3 ATM/ATR DNA-PK AMPK PDPK1 PTEN PI4K PP2A
Other PI3K Inhibitors	GDC-0077 (Inavolisib) SAR405 Quercetin (Sophoretin) LY294002 XL147 analogue Tersolisib (STX-478) Buparlisib (BKM120) 740 Y-P (PDGFR 740Y-P) GO-203 TFA Eganelisib (IPI-549)

Solubility

In vitro
Batch:

DMSO : 5 mg/mL (13.07 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.400mg/ml (1.05mM)	Taking the 1 mL working solution as an example, add 50 μL of 8 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	382.42	Formula	C₁₈H₂₂N₈O₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1382979-44-3	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	RG7666			SMILES	CC1(C2=NC3=C(N2CCO1)N=C(N=C3N4CCOCC4)C5=CN=C(N=C5)N)C

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

Targets/IC₅₀/Ki	PI3Kα (Cell-free assay) 2 nM(Ki app) PI3Kδ (Cell-free assay) 3 nM(Ki app) PI3Kγ (Cell-free assay) 10 nM(Ki app) PI3Kβ (Cell-free assay) 46 nM(Ki app) mTOR (Cell-free assay) 70 nM(Ki app)
In vitro	Paxalisib (GDC-0084) has excellent human metabolic stability in microsomal and hepatocyte incubations and demonstrated inhibition of pAKT, a key signal within the PI3K pathway, in normal brain tissue. This compound is shown to inhibit the proliferation of several glioma cells in vitro with IC50 ranging from 0.3 to 1.1 μM. Its binding to plasma proteins is low, with a free fraction (%) of 29.5±2.7 (n=3) in CD-1 mouse plasma, when tested at 5 μM. Binding to brain tissues from CD-1 mice is higher, with a free fraction of 6.7% (±1; n=3).
In vivo	Paxalisib (GDC-0084) markedly inhibits the PI3K pathway in mouse brain, causing up to 90% suppression of the pAkt signal. It achieves significant tumor growth inhibition of 70% and 40% against the U87 and GS2 orthotopic models, respectively. This compound's distribution throughout the brain and intracranial tumors leads to potent inhibition of the PI3K pathway. It is being evaluated in patients, and exposures reached at tolerated doses are consistent with those associated with efficacious doses in mouse models.
References	[1] https://pubmed.ncbi.nlm.nih.gov/27096040/ [2] https://pubmed.ncbi.nlm.nih.gov/27638506/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-06-23)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT07447076	RECRUITING	Recurrent Atypical Teratoid/Rhabdoid Tumor; Atypical Teratoid/Rhabdoid Tumor (ATRT) of the CNS	Sabine Mueller, MD, PhD	2026-06-17	PHASE2
NCT06208657	RECRUITING	Childhood Cancer; Childhood Solid Tumor; Childhood Brain Tumor; Recurrent Cancer; Refractory Cancer	Australian & New Zealand Children's Haematology/Oncology Group	2024-07-10	PHASE1; PHASE2
NCT07391215	RECRUITING	Malignant Primary Gliomas; Glioblastoma Multiforme (GBM)	Institute of Cancer Research, United Kingdom	2026-01-19	PHASE1; PHASE2
NCT03970447	RECRUITING	Glioblastoma	Global Coalition for Adaptive Research	2019-07-30	PHASE2; PHASE3
NCT05009992	RECRUITING	Diffuse Intrinsic Pontine Glioma; Diffuse Midline Glioma, H3 K27M-Mutant; Recurrent Diffuse Intrinsic Pontine Glioma; Recurrent Diffuse Midline Glioma, H3 K27M-Mutant; Recurrent WHO Grade III Glioma; WHO Grade III Glioma	University of California, San Francisco	2021-10-20	PHASE2
NCT07287202	RECRUITING	Focal Cortical Dysplasia; Tuberous Sclerosis Complex (TSC); Hemimegalencephaly	Sovargen	2026-07-14	PHASE1; PHASE2

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

Paxalisib (GDC-0084) PI3K/mTOR inhibitor

Chemical Structure

Molecular Weight: 382.42