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Pilaralisib (XL147)

Name: Pilaralisib (XL147)
Brand: Selleck Chemicals
SKU: S7645
Rating: 5 (12 reviews)

Catalog No.S7645

For research use only.

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.

CAS No. 934526-89-3

Selleck's Pilaralisib (XL147) has been cited by 12 Publications

3 Customer Reviews

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PI3K Signaling Pathway Map

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

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]

Assay

Methods	Test Index	PMID

Western blot	IGF-1R / AKT / MAPK	22113431
Immunofluorescence	PAK ; phospho-PAK	23915247

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 (from 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 Research:^[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 Research:^[2]	Animal Models: BALB/c nu/nu mice with glioma xenografts Dosages: 100 mg/kg Administration: p.o.

References

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Solubility (25°C)

In vitro	DMSO	100 mg/mL warmed (184.83 mM)
	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

Chemical Information

Molecular Weight	541.02
Formula	C₂₅H₂₅ClN₆O₄S
CAS No.	934526-89-3
Storage	3 years	-20°C	powder
Storage	2 years	-80°C	in solvent
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

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In vivo Formulation Calculator (Clear solution)

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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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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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

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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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