Home PI3K/Akt/mTOR PI3K inhibitor Pilaralisib (XL147)

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Pilaralisib (XL147) PI3K inhibitor

Cat.No.S7645

Pilaralisib (XL147) is a selective and reversible class I PI3K inhibitor for PI3Kα/δ/γ with IC50 of 39 nM/36 nM/23 nM in cell-free assays, and is less potent to PI3Kβ. It has reached Phase 1/2 clinical trials.
Pilaralisib (XL147) PI3K inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 541.02

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Quality Control

Batch: S764501 DMSO]100 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.75%
99.75

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (184.83 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
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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.

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Chemical Information, Storage & Stability

Molecular Weight 541.02 Formula

C25H25ClN6O4S

 Storage (From the date of receipt)
CAS No. 934526-89-3 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CC(C)(C(=O)NC1=CC(=CC=C1)S(=O)(=O)NC2=NC3=CC=CC=C3N=C2NC4=C(C=CC(=C4)OC)Cl)N

Mechanism of Action

Targets/IC50/Ki
PI3Kγ
23 nM
PI3Kβ
36 nM
PI3Kδ
36 nM
PI3Kα
39 nM
In vitro
In Pediatric Preclinical Testing Program (PPTP) cell lines, Pilaralisib (XL147) exhibits cytotoxic activity, with a median relative IC50 value of 10.9 mM (range 2.7 mM to 24.5 mM).
Kinase Assay
In vitro kinase inhibition assays
Kinase activity for PI3K isoforms is measured as the percentage of ATP consumed following the kinase reaction using luciferase–luciferin-coupled chemiluminescence, with ATP concentrations approximately equal to the Km for each respective kinase. Kinase reactions are initiated by combining test compounds, ATP and kinase in a 20 μL volume. PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ final enzyme concentrations are 0.5, 8, 20, and 2 nM, respectively. Of note, 0.5 μL dimethyl sulfoxide (DMSO) containing varying concentrations of this compound is mixed with 10 μL enzyme solution (2×concentration). Kinase reactions are initiated by the addition of 10 μL of liver phosphatidylinositol and ATP solution (2×concentration). Assay concentrations for VPS34, ATP, and phosphatidylinositol are 40 nM, 1 μM, and 5 μM, respectively.
In vivo
In BALB/c nu/nu mice, Pilaralisib (XL147) (100 mg/kg, p.o.) induces tumor growth inhibition for solid glioma xenografts and is well tolerated, with only 0.7% toxicity rate in the treated groups, similar to that observed for control animals. In athymic female mouse, it (100 mg/kg, p.o.) significantly delays tumor growth without significant drug-related toxicity.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/24634413/
  • [5] https://pubmed.ncbi.nlm.nih.gov/23948973/

Applications

Methods Biomarkers Images PMID
Western blot IGF-1R / AKT / MAPK
S7465-WB1
22113431
Immunofluorescence PAK phospho-PAK
S7465-IF1
23915247

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01240460 Completed
Glioblastoma|Astrocytoma Grade IV
Sanofi
 January 2011 Phase 1
NCT01013324 Completed
Endometrial Cancer|Endometrial Neoplasms
Sanofi
 January 2010 Phase 2
NCT00756847 Completed
Cancer|Non-Small Cell Lung Cancer|Endometrial Carcinoma|Ovarian Carcinoma
Sanofi
 September 2008 Phase 1
NCT00704392 Withdrawn
Cancer|Non-small-cell Lung Cancer|Breast Cancer
Exelixis
 June 2008 Phase 1

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