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Pilaralisib (XL147)

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, less potent to PI3Kβ. Phase 1/2.

Pilaralisib (XL147) Chemical Structure

Pilaralisib (XL147) Chemical Structure

CAS: 934526-89-3

Selleck's Pilaralisib (XL147) has been cited by 14 Publications

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Purity & Quality Control

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

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Biological Activity

Description 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, less potent to PI3Kβ. Phase 1/2.
Targets
PI3Kγ [1] PI3Kβ [1] PI3Kδ [1] PI3Kα [1]
23 nM 36 nM 36 nM 39 nM
In vitro
In vitro Pilaralisib exhibits cytotoxic activity in Pediatric Preclinical Testing Program (PPTP) cell lines, with a median relative IC50 value of 10.9 mM (range 2.7 mM to 24.5 mM).[2]
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 the test 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
Cell Research Cell lines BT474 cells
Concentrations 6 μM
Incubation Time 5 days
Method Cell proliferation is measured by using MTT or pre-mixed WST-1 reagent. For MTT/WST-1 assays, 10,000 cells/well are seeded in 96-well plates. 24 h after plating, cells are treated with DMSO or pilaralisib. After 5 days of treatment, MTT/WST-1 assays are performed.
Experimental Result Images Methods Biomarkers Images PMID
Western blot IGF-1R / AKT / MAPK 22113431
Immunofluorescence PAK phospho-PAK 23915247
In Vivo
In vivo In BALB/c nu/nu mice, Pilaralisib (100 mg/kg, p.o.) induces tumor growth inhibition for solid glioma xenografts. Pilaralisib is well tolerated, with only 0.7% toxicity rate in the treated groups, similar to that observed for control animals.[2] In athymic female mouse, Pilaralisib (100 mg/kg, p.o.) significantly delays tumor growth without significant drug-related toxicity.[3]
Animal Research Animal Models BALB/c nu/nu mice with glioma xenografts
Dosages 100 mg/kg
Administration p.o.
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

Chemical lnformation & Solubility

Molecular Weight 541.02 Formula

C25H25ClN6O4S
CAS No. 934526-89-3 SDF Download Pilaralisib (XL147) SDF
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
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (184.83 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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