Referencia número: HY-10303

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PIK-294

2 Cited Publications

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Based on 2 publication(s) in Google Scholar

PIK-294 is a potent p110δ-selective inhibitor with an IC₅₀ of 10 nM.

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Pureza: 99.85%
No. CAS: 900185-02-6
Fòrmula: C₂₈H₂₃N₇O₂
Peso molecular:489.53

Almacenamiento:

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

PIK-294 Chemical Structure

No. CAS: 900185-02-6

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Actividad biológica
- Descripciòn
- IC₅₀ & Target
- In Vitro
Chemical Information
Publications (2)
Solvente y solubilidad
- In Vitro
- In Vivo
Protocolo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

PIK-294 is a potent p110δ-selective inhibitor with an IC₅₀ of 10 nM.

IC₅₀ & Target^[1]

p110δ

10 nM (IC₅₀)

p110γ

160 nM (IC₅₀)

p110β

490 nM (IC₅₀)

p110α

10 μM (IC₅₀)

Ver todos los productos específicos de isoformas PI3K :

In Vitro

Analysis of the specific Class I PI3 Kinase catalytic isoforms p110α (IC₅₀=10 μM), p110β (IC₅₀=0.49 μM), p110δ (IC₅₀=0.01 μM) and p110γ (IC₅₀=0.16 μM) using the inhibitor PIK-294 indicates differential roles in CXCL8-induced neutrophil migration. PIK-294 inhibits both chemokinetic and chemotactic CXCL8-induced migration^[1]. When cells are pre-treated with the PI3Kδ selective inhibitor PIK-294, CXCL8-induced migration in the non-gradient and the gradient assay is significantly inhibited. PIK-294 is used at two concentrations 1 μM and 10 μM. Pre-treatment with 1 μM inhibits migration to a greater extent in the non-gradient assay than in the gradient assay. Pre-treatment with 10 μM inhibits migration to a significantly greater extent than the lower dose in both assays. Prior to stimulation with CXCL8, pre-treatment of the cells with the PI3K inhibitors, Wortmannin (50 nM), PIK-294 (10 μM) and AS-605240 (10 μM) for 2 minutes, cause a reduction in the phosphorylation of Akt. Pre-treatment of cells prior to stimulation with GM-CSF and the DMSO control with the PI3K inhibitors Wortmannin (50 nM), PIK-294 (10 μM) and AS-605240 (10 μM) for 2 minutes, reduce the phosphorylation of Akt (p<0.05 for inhibition of PI3Kδ)^[2].

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

Chemical Information

No. CAS 900185-02-6
Appearance Solid
Peso molecular 489.53
Fòrmula C₂₈H₂₃N₇O₂
Color White to off-white
SMILES

O=C1N(C2=CC=CC=C2C)C(CN3N=C(C(C3=NC=N4)=C4N)C5=CC(O)=CC=C5)=NC6=CC=CC(C)=C16
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

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

Publications (2)

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Cell Rep

Adipocyte PI3K links adipostasis with baseline insulin secretion at fasting through an adipoincretin effect. [Abstract]

2024 Apr 23;43(5):114132. PMID: 38656871
Molecules

In Vitro and in Vivo Activity of mTOR Kinase and PI3K Inhibitors Against Leishmania donovani and Trypanosoma brucei. [Abstract]

2020 Apr 23;25(8):1980. PMID: 32340370

Solvente y solubilidad

In Vitro:

DMSO : 100 mg/mL (204.28 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

2.0428 mL

10.2139 mL

20.4278 mL

5 mM

0.4086 mL

2.0428 mL

4.0856 mL

10 mM

0.2043 mL

1.0214 mL

2.0428 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.

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

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 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.11 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

Protocolo

Cell Assay^[2]

Neutrophils at a concentration of 6×10⁶ cells/mL are pre-treated with 1 μM and 10 μM of the PIK-294 for 30 mins prior to the addition of CXCL8 (100 ng/mL) or 0.5 ng/mL GM-CSF. Then a non-gradient or gradient gel assay depending on the type of migration is performed. The gels are then constructed and the migration studied^[2].

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

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (284 KB)
SDS (420 KB)
- English - EN (420 KB)
- Français - FR (420 KB)
- Deutsch - DE (420 KB)
- Norwegian - NO (420 KB)
- Español - ES (420 KB)
- Swedish - SV (420 KB)
- Italian - IT (420 KB)
- Korean - KR (420 KB)
- Portuguese - PT (420 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)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Knight ZA, et al. A pharmacological map of the PI3-K family defines a role for p110alpha in insulin signaling. Cell. 2006 May 19;125(4):733-47. [Content Brief]

[2]. Martin KJ, et al. The role of phosphoinositide 3-kinases in neutrophil migration in 3D collagen gels. PLoS One. 2015 Feb 6;10(2):e0116250. [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	2.0428 mL	10.2139 mL	20.4278 mL	51.0694 mL
	5 mM	0.4086 mL	2.0428 mL	4.0856 mL	10.2139 mL
	10 mM	0.2043 mL	1.0214 mL	2.0428 mL	5.1069 mL
	15 mM	0.1362 mL	0.6809 mL	1.3619 mL	3.4046 mL
	20 mM	0.1021 mL	0.5107 mL	1.0214 mL	2.5535 mL
	25 mM	0.0817 mL	0.4086 mL	0.8171 mL	2.0428 mL
	30 mM	0.0681 mL	0.3405 mL	0.6809 mL	1.7023 mL
	40 mM	0.0511 mL	0.2553 mL	0.5107 mL	1.2767 mL
	50 mM	0.0409 mL	0.2043 mL	0.4086 mL	1.0214 mL
	60 mM	0.0340 mL	0.1702 mL	0.3405 mL	0.8512 mL
	80 mM	0.0255 mL	0.1277 mL	0.2553 mL	0.6384 mL
	100 mM	0.0204 mL	0.1021 mL	0.2043 mL	0.5107 mL

Keywords

PIK-294

2 Cited Publications

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Publications Citing Use of MedChemExpress (MCE) PIK-294

Ver todos los productos específicos de isoformas PI3K

Actividad biológica

Chemical Information

Publications (2)

Solvente y solubilidad

Protocolo

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

PIK-294 Related Classifications

HY-10303 Related Classifications