For research use only.
CAS No. 934526-89-3
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.
Selleck's Pilaralisib (XL147) has been cited by 10 publications
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I. OMI index decreases in BT474 organoids treated with single and combination therapies at 24 hr. J. OMI index of BT474 organoids treated for 72hr. Red bars denote p<0.05 for treated organoids vs. control. H:trastuzumab (anti-HER2); P:paclitaxel (chemotherapy); XL147 (X).
Cancer Res, 2014, 74(18):5184-94. Pilaralisib (XL147) purchased from Selleck.
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.
Cancer Res, 2014, 74(18):5184-5194.. Pilaralisib (XL147) purchased from Selleck.
Purity & Quality Control
Choose Selective PI3K Inhibitors
|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.|
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).
|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. In athymic female mouse, Pilaralisib (100 mg/kg, p.o.) significantly delays tumor growth without significant drug-related toxicity.|
|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
-  Foster P, et al. Mol Cancer Ther. 2015, 14(4), 931-940.
-  Reynolds CP, et al. Pediatr Blood Cancer. 2013, 60(5), 791-798.
-  Chakrabarty A, et al. Proc Natl Acad Sci U S A. 2012, 109(8), 2718-2723.
|In vitro||DMSO||100 mg/mL warmed (184.83 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
10 mM HCl in sterile water
For best results, use promptly after mixing.
* 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.
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||ul||Number of animals|
|Step 2: Enter the in vivo formulation ()|
|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
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.
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.
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2
Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT01240460||Completed||Drug: XL765 (SAR245409)|Drug: XL147 (SAR245408)||Glioblastoma|Astrocytoma Grade IV||Sanofi||January 2011||Phase 1|
|NCT01013324||Completed||Drug: XL147 (SAR245408)||Endometrial Cancer|Endometrial Neoplasms||Sanofi||January 2010||Phase 2|
|NCT00756847||Completed||Drug: XL147 (SAR245408)|Drug: paclitaxel|Drug: carboplatin||Cancer|Non-Small Cell Lung Cancer|Endometrial Carcinoma|Ovarian Carcinoma||Sanofi||September 2008||Phase 1|
|NCT00704392||Withdrawn||Drug: XL647|Drug: XL147||Cancer|Non-small-cell Lung Cancer|Breast Cancer||Exelixis||June 2008||Phase 1|
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.
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