Art. -Nr.: HY-12235

PI-3065

4 Cited Publications

Kundenbewertung

Based on 4 publication(s) in Google Scholar

PI-3065 is a potent inhibitor of PI3K p110δ, with IC₅₀ and K_i values of 5 nM and 1.5 nM, and exhibits less potent activity against p110α, p110β, p110γ with IC₅₀s of 910, 600, >10000 nM.

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Reinheit: 98.97%
CAS. Nr.: 955977-50-1
Formel: C₂₇H₃₁FN₆OS
Molecular Weight:506.64

Speicherung:

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

PI-3065 Chemical Structure

CAS. Nr.: 955977-50-1

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (4)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

p110δ

5 nM (IC₅₀)

p110β

600 nM (IC₅₀)

p110α

910 nM (IC₅₀)

Alle PI3K Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
Sf21	IC₅₀	1078 nM Compound: PI-3065	Inhibition of human full length recombinant N-terminal His-tagged PI3Kbeta/p85alpha expressed in baculovirus infected Sf21 insect cells Inhibition of human full length recombinant N-terminal His-tagged PI3Kbeta/p85alpha expressed in baculovirus infected Sf21 insect cells	[PMID: 30530193]

In Vitro

PI-3065 exhibits no inhibition of the growth of 4T1 cells, which do not express detectable levels of p110δ^[1].

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

In Vivo

PI-3065 (75 mg/kg, p.o.) inhibits the growth of 4T1 tumours in the BALB/c mice without obvious body weight loss^[1].

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

Chemical Information

CAS. Nr. 955977-50-1
Appearance Solid
Molecular Weight 506.64
Formel C₂₇H₃₁FN₆OS
Color White to off-white
SMILES

FC(C=CC1=C2C=CN1)=C2C3=NC4=C(SC(CN5CCN(CC6CC6)CC5)=C4)C(N7CCOCC7)=N3
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Publications (4)

All WB

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Journal Impact Factor

Nat Commun

Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]

2026 Feb 12;17(1):1214. PMID: 41680175
Sci Signal

Suppression of caspase 8 activity by a coronin 1-PI3Kδ pathway promotes T cell survival independently of TCR and IL-7 signaling. [Abstract]

2021 Dec 21;14(714):eabj0057. PMID: 34932374
Cell Signal

TLR signalling affects sperm mitochondrial function and motility via phosphatidylinositol 3-kinase and glycogen synthase kinase-3α. [Abstract]

2016 Mar;28(3):148-56. PMID: 26658093

PI-3065 purchased from MedChemExpress. Usage Cited in: Cell Signal. 2016 Mar;28(3):148-56. [Abstract]

Inhibition of PI3K p110δ signalling, either by PI3KCD^-/- or using PI3K p110δ inhibitor PI-3065, significantly blocks LPS-induced GSK3α phosphorylation.
Research Square Preprint

2022 Jan.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 25 mg/mL (49.34 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

1.9738 mL

9.8689 mL

19.7379 mL

5 mM

0.3948 mL

1.9738 mL

3.9476 mL

10 mM

0.1974 mL

0.9869 mL

1.9738 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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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 (4.93 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% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.93 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, 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

Protokoll

Animal Administration^[1]

Female WT BALB/c mice are orthotopically inoculated in the mammary fat pad on day 0 with 1×10⁵ 4T1 cells. Drug (75 mg/kg PI-3065, once daily) or vehicle (0.5% methylcellulose with 0.2% Tween 80) is administered by oral gavage from day -1 (administered 12 h prior to tumour cell inoculation). Tumour growth is monitored weekly by caliper measurement or by measuring luminescence using a Xenogen imaging platform. On day 35, mice are euthanized, tumours and peripheral organs extracted for in vitro luminescence measurement, followed by fixation in 4% PFA and H&E staining. KPC mice are allowed to develop advanced lesions of 5-10 mm (determined by ultrasound imaging) before treatment with vehicle or PI-3065 for a total of 14 days.

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 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)
Handling Instructions (2659 KB)

Verweise

[1]. Ali K, et al. Inactivation of PI(3)K p110δ breaks regulatory T-cell-mediated immune tolerance to cancer. Nature. 2014 Jun 19;509(7505):407-11. [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	1.9738 mL	9.8689 mL	19.7379 mL	49.3447 mL
	5 mM	0.3948 mL	1.9738 mL	3.9476 mL	9.8689 mL
	10 mM	0.1974 mL	0.9869 mL	1.9738 mL	4.9345 mL
	15 mM	0.1316 mL	0.6579 mL	1.3159 mL	3.2896 mL
	20 mM	0.0987 mL	0.4934 mL	0.9869 mL	2.4672 mL
	25 mM	0.0790 mL	0.3948 mL	0.7895 mL	1.9738 mL
	30 mM	0.0658 mL	0.3290 mL	0.6579 mL	1.6448 mL
	40 mM	0.0493 mL	0.2467 mL	0.4934 mL	1.2336 mL

Keywords

PI-3065

4 Cited Publications

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Publications Citing Use of MedChemExpress (MCE) PI-3065

Alle PI3K Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (4)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

PI-3065 Related Classifications

HY-12235 Related Classifications