Referencia número: HY-111184

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PIK-108

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PIK-108 is a non-ATP competitive, allosteric p110β/p110δ selective inhibitor.

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Pureza: 99.05%
No. CAS: 901398-68-3
Fòrmula: C₂₂H₂₄N₂O₃
Peso molecular:364.44

Almacenamiento:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

PIK-108 Chemical Structure

No. CAS: 901398-68-3

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Actividad biológica
- Descripciòn
- Cellular Effect
- In Vitro
Chemical Information
Solvente y solubilidad
- In Vitro
- In Vivo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

PIK-108 is a non-ATP competitive, allosteric p110β/p110δ selective inhibitor^[1].

Ver todos los productos específicos de isoformas PI3K :

Cellular Effect

Cell Line	Type	Value	Description	References
PC-3	IC₅₀	3 nM Compound: PIK-108	Inhibition of human PI3Kbeta-mediated Akt phosphorylation at Ser473 residue expressed in PTEN-deficient human PC3 cells by chemiluminescence assay Inhibition of human PI3Kbeta-mediated Akt phosphorylation at Ser473 residue expressed in PTEN-deficient human PC3 cells by chemiluminescence assay	[PMID: 22524426]
PC-3	IC₅₀	3 nM Compound: PIK-108	Inhibition of human PI3Kbeta-mediated Akt phosphorylation at T308 residue expressed in PTEN-deficient human PC3 cells after 2 hrs by Western blot analysis Inhibition of human PI3Kbeta-mediated Akt phosphorylation at T308 residue expressed in PTEN-deficient human PC3 cells after 2 hrs by Western blot analysis	[PMID: 22524426]
PC-3	IC₅₀	3 nM Compound: PIK-108	Inhibition of mTORC2-mediated Akt phosphorylation at Ser473 residue in PTEN-deficient human PC3 cells after 2 hrs by Western blot analysis Inhibition of mTORC2-mediated Akt phosphorylation at Ser473 residue in PTEN-deficient human PC3 cells after 2 hrs by Western blot analysis	[PMID: 22524426]
Sf9	IC₅₀	>10000 nM Compound: PIK-108	Inhibition of N-terminus poly-His tagged human PI3Kgamma expressed in baculovirus infected insect sf9 cells using PI(4,5)P2 as substrate preincubated with compound for 15 mins measured after 10 mins by HTRF assay Inhibition of N-terminus poly-His tagged human PI3Kgamma expressed in baculovirus infected insect sf9 cells using PI(4,5)P2 as substrate preincubated with compound for 15 mins measured after 10 mins by HTRF assay	[PMID: 22524426]
Sf9	IC₅₀	658 nM Compound: PIK-108	Inhibition of poly-His tagged human PI3Kdelta expressed in baculovirus infected insect sf9 cells coexpressing p85alpha using PI(4,5)P2 as substrate preincubated with compound for 15 mins measured after 10 mins by HTRF assay Inhibition of poly-His tagged human PI3Kdelta expressed in baculovirus infected insect sf9 cells coexpressing p85alpha using PI(4,5)P2 as substrate preincubated with compound for 15 mins measured after 10 mins by HTRF assay	[PMID: 22524426]
Sf9	IC₅₀	>10000 nM Compound: PIK-108	Inhibition of N-terminus poly-His tagged human PI3Kalpha expressed in baculovirus infected insect sf9 cells coexpressing p85alpha using PI(4,5)P2 as substrate preincubated with compound for 15 mins measured after 10 mins by HTRF assay Inhibition of N-terminus poly-His tagged human PI3Kalpha expressed in baculovirus infected insect sf9 cells coexpressing p85alpha using PI(4,5)P2 as substrate preincubated with compound for 15 mins measured after 10 mins by HTRF assay	[PMID: 22524426]

In Vitro

PIK-108 (0.1-10 μM; 1 hour) blocks phosphorylation of PKB/Akt^[1].

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

Western Blot Analysis^[1]

Cell Line:

Glioma cell lines expressing wild-type PTEN
Concentration:

0.1, 0.5, 1, 4, and 10 μM
Incubation Time:

1 hour
Result:

Showed variable inhibition of PKB/Akt phosphorylation but exhibited a trend toward reducing PKB/Akt phosphorylation more effectively in mutant PTEN-expressing cell lines than in wild-type PTEN-expressing cell lines.

Chemical Information

No. CAS 901398-68-3
Appearance Solid
Peso molecular 364.44
Fòrmula C₂₂H₂₄N₂O₃
Color White to off-white
SMILES

O=C1C=C(N2CCOCC2)OC3=C(C(NC4=CC=CC=C4)C)C=C(C)C=C13
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvente y solubilidad

In Vitro:

DMSO : 50 mg/mL (137.20 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

2.7439 mL

13.7197 mL

27.4394 mL

5 mM

0.5488 mL

2.7439 mL

5.4879 mL

10 mM

0.2744 mL

1.3720 mL

2.7439 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (5.71 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (5.71 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (5.71 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 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

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (276 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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]. Zachary A Knight, 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]. Jack S Chen, et al. Characterization of structurally distinct, isoform-selective phosphoinositide 3'-kinase inhibitors in combination with radiation in the treatment of glioblastoma. Mol Cancer Ther. 2008 Apr;7(4):841-50. [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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.7439 mL	13.7197 mL	27.4394 mL	68.5984 mL
	5 mM	0.5488 mL	2.7439 mL	5.4879 mL	13.7197 mL
	10 mM	0.2744 mL	1.3720 mL	2.7439 mL	6.8598 mL
	15 mM	0.1829 mL	0.9146 mL	1.8293 mL	4.5732 mL
	20 mM	0.1372 mL	0.6860 mL	1.3720 mL	3.4299 mL
	25 mM	0.1098 mL	0.5488 mL	1.0976 mL	2.7439 mL
	30 mM	0.0915 mL	0.4573 mL	0.9146 mL	2.2866 mL
	40 mM	0.0686 mL	0.3430 mL	0.6860 mL	1.7150 mL
	50 mM	0.0549 mL	0.2744 mL	0.5488 mL	1.3720 mL
	60 mM	0.0457 mL	0.2287 mL	0.4573 mL	1.1433 mL
	80 mM	0.0343 mL	0.1715 mL	0.3430 mL	0.8575 mL
	100 mM	0.0274 mL	0.1372 mL	0.2744 mL	0.6860 mL

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Ver todos los productos específicos de isoformas PI3K

Actividad biológica

Chemical Information

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

PIK-108 Related Classifications

HY-111184 Related Classifications