Pilaralisib (XL147)
Catalog No.S7645
Molecular Weight(MW): 541.02
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.
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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.
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SGC7901 and BGC-823 cells transfected with KLK10 overexpressing plasmid were treated with 10 μg/ml trastuzumab, 5μM XL147, and the combination for 24 hours, p-AKT and total AKT were analyzed by Western blotting
J Cell Biochem, 2018, 119(8):6398-6407. Pilaralisib (XL147) purchased from Selleck.
Purity & Quality Control
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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. | ||||||||
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| 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] |
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| 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
| Kinase Assay: [4] |
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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 |
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| Cell Research:[5] |
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| Animal Research:[2] |
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Solubility (25°C)
| In vitro | DMSO | 100 mg/mL warmed (184.83 mM) |
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| Water | Insoluble | |
| Ethanol | Insoluble | |
| 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. |
0.5mg/mL |
* 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.
Chemical Information
| Molecular Weight | 541.02 |
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| Formula | C25H25ClN6O4S |
| CAS No. | 934526-89-3 |
| Storage | powder |
| in solvent | |
| Synonyms | N/A |
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Clinical Trial Information
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
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| NCT01357330 | Completed | Solid Tumors | Sanofi | May 2011 | Phase 1 |
| NCT01357330 | Completed | Solid Tumors | Sanofi | May 2011 | Phase 1 |
| NCT01240460 | Completed | Glioblastoma|Astrocytoma Grade IV | Sanofi | January 2011 | Phase 1 |
| NCT01240460 | Completed | Glioblastoma|Astrocytoma Grade IV | Sanofi | January 2011 | Phase 1 |
| NCT01082068 | Completed | Breast Cancer | Sanofi | June 2010 | Phase 1|Phase 2 |
| NCT01082068 | Completed | Breast Cancer | Sanofi | June 2010 | Phase 1|Phase 2 |
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.
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