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Pilaralisib

Pilaralisib
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Purity:99.61%
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Pilaralisib

Catalog No. T2365Cas No. 934526-89-3
Pilaralisib (XL-147) is an orally available small molecule that selectively inhibits the activity of phosphoinositide-3 kinase (PI3K). Pilaralisib has been used in trials studying the treatment of Cancer, Lymphoma, Solid Tumors, Glioblastoma, and Breast Cancer, among others.
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Pack SizePriceAvailabilityQuantity
2 mg$45In Stock
5 mg$63In Stock
10 mg$117In Stock
25 mg$197In Stock
50 mg$297In Stock
100 mg$415In Stock
1 mL x 10 mM (in DMSO)$81In Stock
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Product Introduction

Bioactivity
Description
Pilaralisib (XL-147) is an orally available small molecule that selectively inhibits the activity of phosphoinositide-3 kinase (PI3K). Pilaralisib has been used in trials studying the treatment of Cancer, Lymphoma, Solid Tumors, Glioblastoma, and Breast Cancer, among others.
Targets&IC50
PI3Kδ:36 nM, PI3Kβ:36 nM, PI3Kγ:23 nM, PI3Kα:39 nM
In vitro
Pilaralisib exhibits cytotoxic activity in Pediatric PreClinicalal 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]
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 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.(Only for Reference)
AliasSAR245408, XL-147
Chemical Properties
Molecular Weight541.02
FormulaC25H25ClN6O4S
Cas No.934526-89-3
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 93 mg/mL (171.9 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.8484 mL9.2418 mL18.4836 mL92.4180 mL
5 mM0.3697 mL1.8484 mL3.6967 mL18.4836 mL
10 mM0.1848 mL0.9242 mL1.8484 mL9.2418 mL
20 mM0.0924 mL0.4621 mL0.9242 mL4.6209 mL
50 mM0.0370 mL0.1848 mL0.3697 mL1.8484 mL
100 mM0.0185 mL0.0924 mL0.1848 mL0.9242 mL

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