Inhibitor Expert (Inhibitors, Compound Libraries)


Pilaralisib (XL147)

Technical Data

Molecular Weight 541.02 Storage powder


in solvent
CAS No. 934526-89-3 Synonyms N/A
Chemical Name N-(3-{[(3-{[2-chloro-5-(methoxy)phenyl]amino}quinoxalin-2-yl)amino]sulfonyl}phenyl)-2-methylalaninamide
Solubility (25°C) * In vitro DMSO 100 mg/mL warmed (184.83 mM)
Water Insoluble
Ethanol Insoluble
In vivo 10 mM HCl in sterile water 0.5mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

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.
PI3Kγ [1] PI3Kβ [1] PI3Kδ [1] PI3Kα [1]
23 nM 36 nM 36 nM 39 nM
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]
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]

Protocol (Only for Reference)

Kinase Assay: [4]
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 Assay: [5]
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.
Animal Study: [2]
Animal Models BALB/c nu/nu mice with glioma xenografts
Formulation 10 mM HCl in sterile water
Dosages 100 mg/kg
Administration p.o.


Customer Product Validation

Data from [Data independently produced by , , Cancer Res, 2014, 74(18):5184-5194.]

G, tumor growth response of HR6 tumors grown in athymic nude mice and treated with single and combination treatments. H, table of earliest detectable (P < 0.05) reduction in tumor size for control versus treated mice. ^, tumors that initially shrank and then grew; NS, not significant. I, OMI index initially decreases in HR6 organoids treated with paclitaxel, XL147, and combination therapies at 24 hours. J, OMI index of HR6 organoids treated for 72 hours. Red bars, significant reductions in OMI index; P< 0.05, for treated organoids versus control. Blue bars, significant increases in OMIindex;P< 0.05, for treated organoids versus control.

Pilaralisib (XL147) has been referenced in publications.



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Chemical Structure

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