Cat. No.: HY-16526

Pilaralisib

(Synonyms: XL-147; SAR245408)

6 Cited Publications

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Based on 6 publication(s) in Google Scholar

Pilaralisib (XL147; SAR245408) is a potent and highly selective class I PI3Ks inhibitor with IC₅₀s of 39 nM, 383 nM, 23 nM and 36 nM for PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ.

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Pureté: 98.81%
CAS No.: 934526-89-3
Formule: C₂₅H₂₅ClN₆O₄S
Masse moléculaire:541.02

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Pilaralisib Chemical Structure

CAS No.: 934526-89-3

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (6)
Solvant et solubilité
- In Vitro
- In Vivo
Protocole
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

Pilaralisib (XL147; SAR245408) is a potent and highly selective class I PI3Ks inhibitor with IC₅₀s of 39 nM, 383 nM, 23 nM and 36 nM for PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ.

IC₅₀ & Target^[1]

PI3Kγ

23 nM (IC₅₀)

PI3Kδ

36 nM (IC₅₀)

PI3Kα

39 nM (IC₅₀)

PI3Kβ

383 nM (IC₅₀)

Vps34

6974 nM (IC₅₀)

DNA-PK

4750 nM (IC₅₀)

Voir tous les produits spécifiques à Isoform PI3K :

In Vitro

Pilaralisib (XL147) displays potent inhibitory activity against Class I PI3K isoforms p110α, p110δ, and p110γ, with IC₅₀s of 39, 36, and 23 nM, respectively. Pilaralisib (XL147) is less potent against the remaining Class I isoform, p110β, with an IC₅₀ value of 383 nM. The IC₅₀ value for inhibition of PI3Kα by Pilaralisib (XL147) is determined at various concentrations of ATP, revealing XL147 to be an ATP-competitive inhibitor with an equilibrium inhibition constant (K_i) value of 42 nM. Pilaralisib (XL147) has relatively weak inhibitory activity toward the class III PI3K vacuolar sorting protein 34 (VPS34; IC₅₀ value of ~7.0 M) and the PI3K-related DNA-dependent protein kinase (DNA-PK; IC₅₀ value of 4.75 μM). In an mTOR kinase immunoprecipitation assay using cell lysates, Pilaralisib (XL147) does not inhibit mTOR activity toward the physiologic substrate protein eukaryotic translation initiation factor 4E-binding protein 1 (4EBP1; IC₅₀>15 μM). Consistent with its inhibitory activity against purified PI3K proteins, Pilaralisib (XL147) inhibits EGF-induced PIP₃ production in PC-3 and MCF7 cells in serum-free medium with IC₅₀s of 220 and 347 nM, respectively. The ability of Pilaralisib (XL147) to inhibit phosphorylation of key signaling proteins downstream of PI3K is examined by assessing its effects on EGF-stimulated phosphorylation of AKT and on nonstimulated phosphorylation of S6 in PC-3 cells in serum-free media by cell-based ELISA. Pilaralisib (XL147) inhibits these activities with IC₅₀s of 477 and 776 nM, respectively^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

The ability of Pilaralisib (XL147) to inhibit this endogenous phosphorylation of AKT, p70S6K, and S6 is examined following a single oral dose of 10, 30, 100, or 300 mg/kg. The tumors are harvested 4, 24, or 48 hours postdose and homogenized in lysis buffer. Tumor lysates from each animal (n=4) are then pooled for each group and analyzed for levels of total and phosphorylated AKT, p70S6K, and S6 by Western immunoblotting. Administration of Pilaralisib (XL147) causes a dose-dependent decrease in phosphorylation of AKT, p70S6K, and S6 in the tumors, reaching a maximum of 81% inhibition of AKT phosphorylation at 300 mg/kg at 4 hours. The dose-response relationships derived from the 4-hour time point predict 50% inhibition of AKT, p70S6K, and S6 phosphorylation at doses of approximately 100 mg/kg (pAKT^T308), 54 mg/kg (pAKT^S473), 71 mg/kg (p-p70S6K), and 103 mg/kg (pS6). The inhibition of AKT, p70S6K, and S6 phosphorylation in MCF7 tumors following a 100 mg/kg dose of Pilaralisib (XL147) is maximal at 4 hours, reaching 55% to 75%; however, the level of inhibition decreased to 8% to 45% by 24 hours, and only minimal or no inhibition was evident by 48 hours. Following a 300 mg/kg dose of Pilaralisib (XL147), inhibition is also maximal at 4 hours (65%-81%). However, in contrast with the 100 mg/kg dose, inhibition at 24 hours (51%-78%) is almost comparable with that seen at 4 hours, and partial inhibition (25%-51%) persisted through 48 hours^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 934526-89-3
Appearance Solid
Masse moléculaire 541.02
Formule C₂₅H₂₅ClN₆O₄S
Color Light yellow to yellow
SMILES

CC(C)(N)C(NC1=CC=CC(S(=O)(NC2=NC3=CC=CC=C3N=C2NC4=CC(OC)=CC=C4Cl)=O)=C1)=O
Synonyms

XL-147; SAR245408
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (6)

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Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
Cell Syst

Torin2 Exploits Replication and Checkpoint Vulnerabilities to Cause Death of PI3K-Activated Triple-Negative Breast Cancer Cells. [Abstract]

2020 Jan 22;10(1):66-81.e11. PMID: 31812693
Immunotargets Ther

2026 Jan 21;15:1-19.
Immunotargets Ther

Upregulated BLM and RECQL4 in Osteosarcoma: Association with Poor Prognosis, Immune Cell Infiltration, and Inhibitory Effects of Sphingosine Kinase 1 Inhibitor II/Pilaralisib. [Abstract]

2026 Jan 22:15:569823. PMID: 41878019
bioRxiv

2024 September 07.
Methods Mol Biol

Methods for High-throughput Drug Combination Screening and Synergy Scoring. [Abstract]

2018:1711:351-398. PMID: 29344898

Solvant et solubilité

In Vitro:

DMSO : ≥ 100 mg/mL (184.84 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.8484 mL

9.2418 mL

18.4836 mL

5 mM

0.3697 mL

1.8484 mL

3.6967 mL

10 mM

0.1848 mL

0.9242 mL

1.8484 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (4.62 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.5 mg/mL (4.62 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocole

Cell Assay^[1]

MCF7 human mammary carcinoma cells and PC-3 human prostate adenocarcinoma cells are maintained in culture conditions at 37°C under 5% CO₂. For PI3K pathway status assessment following EGF treatment, the culture medium is replaced with test compounds dissolved in serum-free DMEM containing 0.3% DMSO. After incubation for 3 hours, cells are stimulated with 100 ng/mL of EGF for 10 minutes and Western immunoblot analysis of cell lysates is performed. Assessment of mTOR pathway status in Ramos cells is performed. Cellular proliferation is assessed using the Cell Proliferation ELISA, bromodeoxyuridine (BrdUrd) chemiluminescence kit. Cytotoxicity, apoptosis (caspases-3/7), anchorage-independent growth, and PC-3 cell migration assays are performed. Hepatocyte growth factor (HGF)-induced chemotaxis is assessed. Theendothelial cell tube formation assay is performed, with minor modifications. Total tube length is quantified with Image Pro Plus software^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[1]

Mice^[1]
Female athymic nude mice and male nude mice are used. Tumor cells are cultured and established as xenografts in mice, and body and tumor weights assessed. Statistical significance is determined using the two-tailed Student ttest (significance defined as P<0.05). Pilaralisib (XL147) is formulated in sterile water/10 mmol/L HCl or water and administered at the indicated doses and regimens by oral gavage at a dose volume of 10 mL/kg.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (285 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Foster P, et al. The Selective PI3K Inhibitor XL147 (SAR245408) Inhibits Tumor Growth and Survival and Potentiates the Activity of Chemotherapeutic Agents in Preclinical Tumor Models. Mol Cancer Ther. 2015 Apr;14(4):931-40. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.8484 mL	9.2418 mL	18.4836 mL	46.2090 mL
	5 mM	0.3697 mL	1.8484 mL	3.6967 mL	9.2418 mL
	10 mM	0.1848 mL	0.9242 mL	1.8484 mL	4.6209 mL
	15 mM	0.1232 mL	0.6161 mL	1.2322 mL	3.0806 mL
	20 mM	0.0924 mL	0.4621 mL	0.9242 mL	2.3105 mL
	25 mM	0.0739 mL	0.3697 mL	0.7393 mL	1.8484 mL
	30 mM	0.0616 mL	0.3081 mL	0.6161 mL	1.5403 mL
	40 mM	0.0462 mL	0.2310 mL	0.4621 mL	1.1552 mL
	50 mM	0.0370 mL	0.1848 mL	0.3697 mL	0.9242 mL
	60 mM	0.0308 mL	0.1540 mL	0.3081 mL	0.7702 mL
	80 mM	0.0231 mL	0.1155 mL	0.2310 mL	0.5776 mL
	100 mM	0.0185 mL	0.0924 mL	0.1848 mL	0.4621 mL

Keywords

Pilaralisib

6 Cited Publications

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Pilaralisib

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Publications Citing Use of MedChemExpress (MCE) Pilaralisib

Voir tous les produits spécifiques à Isoform PI3K

Activité biologique

Chemical Information

Publications (6)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Pilaralisib Related Classifications

HY-16526 Related Classifications