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Quercetin Dihydrate PI3K inhibitor

Name: Quercetin Dihydrate
Brand: Selleck Chemicals
SKU: S2347
Availability: InStock
Rating: 5 (9 reviews)

Cat.No.S2347

Quercetin (Sophoretin), a polyphenolic flavonoid found in a wide variety of plant-based foods, such as apples, onions, berries, and red wine, is utilized in many different cultures for their nervous system and anticancer effects. Quercetin (dihydrate), a natural flavonoid, is a stimulator of recombinant SIRT1 and a PI3K inhibitor with IC50s of 2.4 μM, 3.0 μM and 5.4 μM for PI3K γ, PI3K δ and PI3K β, respectively.

Chemical Structure

Molecular Weight: 338.27

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Quality Control

Batch: Purity: 99.06%

99.06

Related Targets	Akt mTOR GSK-3 ATM/ATR DNA-PK AMPK PDPK1 PTEN PP2A PDK
Other PI3K Inhibitors	LY294002 Buparlisib (BKM120) SAR405 Eganelisib (IPI-549) XL147 analogue Paxalisib (GDC-0084) Tersolisib (STX-478) 3-Methyladenine (3-MA) Dactolisib (BEZ235) Pictilisib (GDC-0941)

Solubility

In vitro
Batch:

DMSO : 67 mg/mL (198.06 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 17 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	7.500mg/ml (22.17mM)	Taking the 1 mL working solution as an example, add 50 μL of 150 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.300mg/ml (0.89mM)	Taking the 1 mL working solution as an example, add 50 μL of 6 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	338.27	Formula	C₁₅H₁₀O₇.2H₂O	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	6151-25-3	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	Sophoretin			Smiles	C1=CC(=C(C=C1C2=C(C(=O)C3=C(C=C(C=C3O2)O)O)O)O)O.O.O

Mechanism of Action

Targets/IC₅₀/Ki	SIRT1 PI3Kγ (Cell-free assay) 2.4 μM PI3Kδ (Cell-free assay) 3.0 μM PI3Kβ (Cell-free assay) 5.4 μM
In vitro	Quercetin, a polyphenolic flavonoid found in a wide variety of plant-based foods, such as apples, onions, berries, and red wine, is utilized in many different cultures for their nervous system and anticancer effects. The pharmacological activities of quercetin that modulate antioxidation/oxidation/kinase-signaling pathways might be differentially elicited in neurons compared with malignant cells, ultimately promoting cell survival or death in a cell type- and metabolism-specific manner. Whereas the broad antioxidation and anti-inflammatory activities of quercetin are important for neuronal survival, the oxidative, kinase- and cell cycle-inhibitory, apoptosis-inducing effects of quercetin are essential for its anticancer effects.
In vivo	LD50: Mice 159mg/kg (i.g.)
References	[1] https://pubmed.ncbi.nlm.nih.gov/22820241/ [2] https://pubmed.ncbi.nlm.nih.gov/21845161/ [3] https://pubmed.ncbi.nlm.nih.gov/19686810/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT06003270	Recruiting	Chronic Obstructive Pulmonary Disease\|Emphysema\|Chronic Bronchitis With Airway Obstruction	Temple University\|National Center for Complementary and Integrative Health (NCCIH)\|Quercegen Pharmaceuticals	November 1 2023	Phase 2
NCT04907253	Active not recruiting	Coronary Artery Disease	Montreal Heart Institute	June 4 2021	Phase 2
NCT04474626	Withdrawn	Sickle Cell Disease\|Sickle Cell-Beta0-Thalassemia	Jeffrey Zwicker MD\|Quercegen Pharmaceuticals\|Dana-Farber Cancer Institute	December 2020	Phase 2
NCT04063124	Completed	Alzheimer Disease	The University of Texas Health Science Center at San Antonio\|Mayo Clinic	February 14 2020	Phase 1\|Phase 2
NCT03989271	Recruiting	Chronic Obstructive Pulmonary Disease	Temple University\|National Institutes of Health (NIH)\|Quercegen Pharmaceuticals\|National Center for Complementary and Integrative Health (NCCIH)	October 1 2019	Phase 1\|Phase 2

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