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

PI3K/Akt/mTOR-IN-2 is a PI3K/AKT/mTOR pathway inhibitor. PI3K/Akt/mTOR-IN-2 possess anti-cancer effects and selectivity against MDA-MB-231 cells with IC50 value of 2.29 μM. PI3K/Akt/mTOR-IN-2 can induce cancer cell cycle arrest and apoptosis.

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PI3K/Akt/mTOR-IN-2 Chemical Structure

PI3K/Akt/mTOR-IN-2 Chemical Structure

CAS No. : 2757804-89-8

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Based on 2 publication(s) in Google Scholar

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Description

PI3K/Akt/mTOR-IN-2 is a PI3K/AKT/mTOR pathway inhibitor. PI3K/Akt/mTOR-IN-2 possess anti-cancer effects and selectivity against MDA-MB-231 cells with IC50 value of 2.29 μM. PI3K/Akt/mTOR-IN-2 can induce cancer cell cycle arrest and apoptosis[1].

IC50 & Target

IC50: 2.29 μM (PI3K/AKT/mTOR) in MDA-MB-231[1]

In Vitro

PI3K/Akt/mTOR-IN-2 (compound 23) (0.5 - 100 μM; 72 hours) exhibits effective anti-cancer activity with IC50s of 2.29 - 24.63 μM, of which, IC50 in MDA-MB-231 is 2.29 μM[1].
PI3K/Akt/mTOR-IN-2 (1 μM, 2 μM and 4 μM; 24 hours) induces growth inhibition of MDA-MB-231 cells by cell cycle arrest at G0/G1[1].
PI3K/Akt/mTOR-IN-2 (1 μM, 2 μM and 4 μM; 24, 48 and 72 hours) induces apoptosis in MDA-MB-231 cells with both dose- and time-dependent manners[1].
PI3K/Akt/mTOR-IN-2 (1 μM, 2 μM and 4 μM; 48 hours) increases the expression of Bax, and decreases the expression of Bcl-2 in MDA-MB-231 cells[1].
PI3K/Akt/mTOR-IN-2 (1 μM, 2 μM and 4 μM; 24 hours) induces mitochondria-dependent apoptosis in MDA-MB-231 cells through disruption of MMP, accumulation of ROS, depletion of GSH and elevation of intracellular Ca2+[1].

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

Cell Proliferation Assay

Cell Line: PC3, BGC-823, A549, MCF-7, MDA-MB-231 cells and MCF-10A cells[1]
Concentration: 0.5 - 100 μM
Incubation Time: 72 hours
Result: Exhibited effective anti-cancer activity with IC50s of 2.29 - 24.63 μM, of which, IC50 in MDA-MB-231 was 2.29 μM.

Cell Cycle Analysis

Cell Line: MDA-MB-231[1]
Concentration: 1 μM, 2 μM and 4 μM
Incubation Time: 24 hours
Result: Induced growth inhibition of MDA-MB-231 cells by cell cycle arrest at G0/G1.

Apoptosis Analysis

Cell Line: MDA-MB-231[1]
Concentration: 1 μM, 2 μM and 4 μM
Incubation Time: 24, 48 and 72 hours
Result: Induced apoptosis in MDA-MB-231 cells with both dose- and time-dependent manners.

Western Blot Analysis

Cell Line: MDA-MB-231[1]
Concentration: 1 μM, 2 μM and 4 μM
Incubation Time: 48 hours
Result: Increased the expression of Bax, and decreased the expression of Bcl-2
Molecular Weight

285.29

Formula

C17H13F2NO

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

FC1=CC(F)=CC(C2OCCC3=C2NC4=C3C=CC=C4)=C1

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 : ≥ 100 mg/mL (350.52 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.5052 mL 17.5260 mL 35.0521 mL
5 mM 0.7010 mL 3.5052 mL 7.0104 mL
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* 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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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 3.5052 mL 17.5260 mL 35.0521 mL 87.6301 mL
5 mM 0.7010 mL 3.5052 mL 7.0104 mL 17.5260 mL
10 mM 0.3505 mL 1.7526 mL 3.5052 mL 8.7630 mL
15 mM 0.2337 mL 1.1684 mL 2.3368 mL 5.8420 mL
20 mM 0.1753 mL 0.8763 mL 1.7526 mL 4.3815 mL
25 mM 0.1402 mL 0.7010 mL 1.4021 mL 3.5052 mL
30 mM 0.1168 mL 0.5842 mL 1.1684 mL 2.9210 mL
40 mM 0.0876 mL 0.4382 mL 0.8763 mL 2.1908 mL
50 mM 0.0701 mL 0.3505 mL 0.7010 mL 1.7526 mL
60 mM 0.0584 mL 0.2921 mL 0.5842 mL 1.4605 mL
80 mM 0.0438 mL 0.2191 mL 0.4382 mL 1.0954 mL
100 mM 0.0351 mL 0.1753 mL 0.3505 mL 0.8763 mL
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    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.

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