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Pilaralisib

SKU: orb1305590

Description

Pilaralisib (XL-147) is a selective, orally bioavailable phosphoinositide-3 kinase (PI3K) inhibitor. It has been widely employed in preclinical and clinical research, including in vitro cell-based assays and in vivo xenograft models, to investigate its therapeutic potential in cancers such as breast cancer, lymphoma, and glioblastoma.

Research Area

Signal Transduction

Images & Validation

Key Properties

CAS Number934526-89-3
MW541.02
Purity99.61% (May vary between batches)
FormulaC25H25ClN6O4S
SMILESCOc1ccc(Cl)c(Nc2nc3ccccc3nc2NS(=O)(=O)c2cccc(NC(=O)C(C)(C)N)c2)c1
TargetPI3K
SolubilityEthanol:< 1 mg/mL (insoluble or slightly soluble);DMSO:93 mg/mL (171.9 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (6.1 mM)

Bioactivity

Target IC50
PI3Kγ:23 nM|PI3Kα:39 nM|DNA-PK:4750 nM|PI3Kβ:36 nM|VPS34:6974 nM|PI3Kδ:36 nM
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.
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).
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)

Storage & Handling

StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

Inhibitor, inhibit, SAR 245408, SAR245408, SAR-245408, PI3K, Phosphoinositide 3-kinase, XL 147, XL-147, XL147, PI3Kδ, PI3Kβ, PI3Kγ, PI3Kα, Pilaralisib

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Key Properties

No computed properties available.

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Pilaralisib (orb1305590)

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% DMSO +
%+
% Tween 80 +
%

Available Sizes

Select a size below

2 mg
$ 80.00
5 mg
$ 110.00
1 ml x 10 mM (in DMSO)
$ 120.00
10 mg
$ 140.00
25 mg
$ 220.00
50 mg
$ 300.00
100 mg
$ 460.00
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