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Pilaralisib

Catalog No. T2365   CAS 934526-89-3
Synonyms: SAR245408, XL-147

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.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
Pilaralisib Chemical Structure
Pilaralisib, CAS 934526-89-3
Pack Size Availability Price/USD Quantity
2 mg In stock $ 45.00
5 mg In stock $ 63.00
10 mg In stock $ 117.00
25 mg In stock $ 197.00
50 mg In stock $ 297.00
100 mg In stock $ 415.00
1 mL * 10 mM (in DMSO) In stock $ 81.00
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Purity: 99.61%
Purity: 98.51%
Purity: 98.24%
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Biological Description
Chemical Properties
Storage & Solubility Information
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 PI3Kγ:23 nM, PI3Kα:39 nM, PI3Kβ:36 nM, PI3Kδ:36 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)
Synonyms SAR245408, XL-147
Molecular Weight 541.02
Formula C25H25ClN6O4S
CAS No. 934526-89-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 93 mg/mL (171.9 mM)

TargetMolReferences and Literature

1. Foster P, et al. Mol Cancer Ther. 2015, 14(4), 931-940. 2. Reynolds CP, et al. Pediatr Blood Cancer. 2013, 60(5), 791-798. 3. Chakrabarty A, et al. Proc Natl Acad Sci U S A. 2012, 109(8), 2718-2723. 4. Yu P, et al. Mol Cancer Ther. 2014, 13(5), 1078-1091. 5. Rexer BN, et al. Clin Cancer Res. 2013, 19(19), 5390-5401.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Drug Library Anti-Cancer Active Compound Library Anti-Cancer Clinical Compound Library Antidepressant Compound Library Neural Regeneration Compound Library Anti-Aging Compound Library Bioactive Compounds Library Max Anti-Obesity Compound Library Oxidation-Reduction Compound Library NO PAINS Compound Library

Related Products

Related compounds with same targets
PI3Kγ inhibitor 2 Parsaclisib TG 100713 Vps34-IN-1 Vps34-IN-2 PI3K-IN-46 Omipalisib PI3K/Akt/mTOR-IN-2

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Keywords

Pilaralisib 934526-89-3 PI3K/Akt/mTOR signaling PI3K inhibit XL147 Phosphoinositide 3-kinase Inhibitor SAR245408 SAR-245408 SAR 245408 XL 147 XL-147 inhibitor

 

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