2. PI3K/Akt/mTOR Apoptosis
  3. PI3K Akt Apoptosis
  4. PI3K/AKT-IN-1

PI3K/AKT-IN-1 is an effective PI3K/AKT dual inhibitor (IC50 of 6.99, 4.01 and 3.36 μM for PI3Kγ, PI3Kδ and AKT, respectively). PI3K/AKT-IN-1 has anticancer activity and acts by inhibiting PI3K/AKT axis and inducing caspase 3 dependent apoptosis.

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PI3K/AKT-IN-1 Chemical Structure

PI3K/AKT-IN-1 Chemical Structure

CAS No. : 3033069-84-7

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Based on 7 publication(s) in Google Scholar

PI3K/AKT-IN-1 Related Antibodies

Top Publications Citing Use of Products

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  • Biological Activity

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Description

PI3K/AKT-IN-1 is an effective PI3K/AKT dual inhibitor (IC50 of 6.99, 4.01 and 3.36 μM for PI3Kγ, PI3Kδ and AKT, respectively). PI3K/AKT-IN-1 has anticancer activity and acts by inhibiting PI3K/AKT axis and inducing caspase 3 dependent apoptosis[1].

IC50 & Target[1]

PI3Kγ

6.99 μM (IC50)

PI3Kδ

4.01 μM (IC50)

In Vitro

PI3K/AKT-IN-1 (compound 7f) (0.04-100 µM; 48 hours) has high cytotoxic activity on both cell lines with better activity on leukaemia cell line (K562 IC50=2.62 µM) than on the breast cancer cell line (MCF-7 IC50=3.22 µM)[1].
PI3K/AKT-IN-1 (2.62 µM) can promote S-phase cell cycle arrest and apoptosis induction in K562 cells[1].
PI3K/AKT-IN-1 (2.62 µM; 48 hours) causes an increase in the percentage of Annexin-V positive apoptotic cells both in the early and late stage[1].
PI3K/AKT-IN-1 (2.62 µM; 48 hours) markedly reduces the expression of PI3K, AKT, Cyclin D1 and NF-κB[1].

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

PI3K/AKT-IN-1 Related Antibodies

Cell Cytotoxicity Assay

Cell Line: MCF-7 and K562 cells[1]
Concentration: 0.04-100 µM
Incubation Time: 48 hours
Result: Demonstrated high cytotoxic activity on both cell lines with better activity on leukaemia cell line (K562 IC50=2.62 µM) than on the breast cancer cell line (MCF-7 IC50=3.22 µM).

Cell Cycle Analysis

Cell Line: K562 cells[1]
Concentration: 2.62 µM
Incubation Time:
Result: Promoted S-phase cell cycle arrest and apoptosis induction.

Apoptosis Analysis

Cell Line: K562 cells[1]
Concentration: 2.62 µM
Incubation Time: 48 hours
Result: Caused an increase in the percentage of Annexin-V positive apoptotic cells both in the early and late stage.

Western Blot Analysis

Cell Line: K562 cells[1]
Concentration: 2.62 µM
Incubation Time: 48 hours
Result: Markedly reduced the expression of PI3K, p-PI3K, AKT, p-AKT, Cyclin D1 and NF-κB.
In Vivo

PI3K/AKT-IN-1 (2000 mg/kg; p.o.; single) is non-toxic and is well tolerated by experimental animals[1].

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

Animal Model: Female rats (180-200g)[1]
Dosage: 2000 mg/kg
Administration: p.o.; single
Result: The median lethal dose (LD50) was greater than the test dose (2000 mg/kg).
Molecular Weight

465.52

Formula

C23H23N5O4S
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

N#CC1=C(N/N=C/C2=CC(OC)=C(OC)C(OC)=C2)N=C(SC)N=C1C3=CC=C(OC)C=C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (107.41 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1481 mL 10.7407 mL 21.4814 mL
5 mM 0.4296 mL 2.1481 mL 4.2963 mL
View the Complete Stock Solution Preparation Table

* 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.

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

Mass
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

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C2

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V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

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g

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* 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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1481 mL 10.7407 mL 21.4814 mL 53.7034 mL
5 mM 0.4296 mL 2.1481 mL 4.2963 mL 10.7407 mL
10 mM 0.2148 mL 1.0741 mL 2.1481 mL 5.3703 mL
15 mM 0.1432 mL 0.7160 mL 1.4321 mL 3.5802 mL
20 mM 0.1074 mL 0.5370 mL 1.0741 mL 2.6852 mL
25 mM 0.0859 mL 0.4296 mL 0.8593 mL 2.1481 mL
30 mM 0.0716 mL 0.3580 mL 0.7160 mL 1.7901 mL
40 mM 0.0537 mL 0.2685 mL 0.5370 mL 1.3426 mL
50 mM 0.0430 mL 0.2148 mL 0.4296 mL 1.0741 mL
60 mM 0.0358 mL 0.1790 mL 0.3580 mL 0.8951 mL
80 mM 0.0269 mL 0.1343 mL 0.2685 mL 0.6713 mL
100 mM 0.0215 mL 0.1074 mL 0.2148 mL 0.5370 mL
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PI3K/AKT-IN-1 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PI3K/AKT-IN-13033069-84-7PI3KAktApoptosisPhosphoinositide 3-kinasePKBProtein kinase BPyrimidine-5-carbonitrileleukaemiaBreast cancerLeukaemia K562MCF-7PI3K/AKT pathwayDual inhibitorInhibitorinhibitorinhibit

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