1. PI3K/Akt/mTOR
  2. PI3K mTOR
  3. PI3K/mTOR Inhibitor-4

PI3K/mTOR Inhibitor-4 is an orally active pan-class I PI3K/mTOR inhibitor. PI3K/mTOR Inhibitor-4 has enzymatic inhibition activity for PI3Kα, PI3Kγ, PI3Kδ and mTOR with IC50 values of 0.63 nM, 22 nM, 9.2 nM and 13.85 nM, respectively. PI3K/mTOR Inhibitor-4 can be used for the research of cancer.

For research use only. We do not sell to patients.

PI3K/mTOR Inhibitor-4 Chemical Structure

PI3K/mTOR Inhibitor-4 Chemical Structure

CAS No. : 2361215-32-7

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Based on 1 publication(s) in Google Scholar

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Description

PI3K/mTOR Inhibitor-4 is an orally active pan-class I PI3K/mTOR inhibitor. PI3K/mTOR Inhibitor-4 has enzymatic inhibition activity for PI3Kα, PI3Kγ, PI3Kδ and mTOR with IC50 values of 0.63 nM, 22 nM, 9.2 nM and 13.85 nM, respectively. PI3K/mTOR Inhibitor-4 can be used for the research of cancer[1].

IC50 & Target[1]

PI3Kα

0.63 nM (IC50)

PI3Kδ

9.2 nM (IC50)

mTOR

13.85 nM (IC50)

PI3Kβ

94.54 nM (IC50)

PI3Kγ

22 nM (IC50)

In Vitro

PI3K/mTOR Inhibitor-4 (compound 8d-1) has enzymatic inhibition activity for PI3Kα, PI3Kδ, mTOR, PI3Kβ and PI3Kγ with IC50 values of 0.63 nM, 9.2 nM, 13.85 nM, 94.54 nM and 22 nM, respectively[1].
PI3K/mTOR Inhibitor-4 shows potent anti-proliferation activity in A549, Hela, HCT-116, HepG2, A375 and MCF-7 cells with IC50 values of 1.35 nM, 1.22 nM, 13.44 nM, 1.08 nM, 18.4 nM and 8.26 nM, respectively[1].
PI3K/mTOR Inhibitor-4 (2.5-10 µM; 24 h) inhibits the PI3K/AKT/mTOR pathway[1].

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

Cell Viability Assay[1]

Cell Line: PC12 and LO2 cells
Concentration: 0.625-20 µM
Incubation Time: 72 h
Result: Showed low toxicity in concentrations from 0.625 µM to 20 µM.

Western Blot Analysis[1]

Cell Line: Hela cells
Concentration: 2.5, 5 and 10 µM
Incubation Time: 24 h
Result: Dose-dependently decreased the level of phosphorylation of AKT and its downstream target S6 in Hela cell line.
In Vivo

PI3K/mTOR Inhibitor-4 (compound 8d-1) (i.v., oral; 1mg/kg, 10 mg/kg) displays favorable pharmacokinetic parameters in Sprague−Dawley rats[1].
PI3K/mTOR Inhibitor-4 (oral; 10-50 mg/kg) shows significant efficiency in Hela/A549 tumor xenograft models without causing significant weight loss and toxicity[1].

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

Animal Model: SD rats (male; 200-220 g)[1]
Dosage: 1, 10 mg/kg
Administration: Intravenous, oral
Result:
IV (1 mg/kg) PO (10 mg/kg)
CL (ml/min/kg) Vss (ml/kg) Tmax (h) Cmax (ng/ml) AUCinf (ng*h/ml) t1/2 (h) F(%)
8.6 1199.81 2.67 886.67 4753.35 1.78 24.1
Animal Model: BALB/c nude mice (female; 6-7 weeks; 18-22 g)[1]
Dosage: 10, 20, 40, 50 mg/kg/d (Hela model) and 20, 40 mg/kg/d (A549 model)
Administration: Oral
Result: Inhibited the growth of xenograft tumors in a dose-dependent manner.
Molecular Weight

535.54

Formula

C27H22FN3O6S

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

FC1=CC=C(S(NC2=CC(C3=CC=C(OCC(N4C5=CC=C(OC)C=C5)=O)C4=C3)=CN=C2OC)(=O)=O)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (466.82 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 1.8673 mL 9.3364 mL 18.6727 mL
5 mM 0.3735 mL 1.8673 mL 3.7345 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 (protect from light). 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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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 (protect from light). 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 1.8673 mL 9.3364 mL 18.6727 mL 46.6819 mL
5 mM 0.3735 mL 1.8673 mL 3.7345 mL 9.3364 mL
10 mM 0.1867 mL 0.9336 mL 1.8673 mL 4.6682 mL
15 mM 0.1245 mL 0.6224 mL 1.2448 mL 3.1121 mL
20 mM 0.0934 mL 0.4668 mL 0.9336 mL 2.3341 mL
25 mM 0.0747 mL 0.3735 mL 0.7469 mL 1.8673 mL
30 mM 0.0622 mL 0.3112 mL 0.6224 mL 1.5561 mL
40 mM 0.0467 mL 0.2334 mL 0.4668 mL 1.1670 mL
50 mM 0.0373 mL 0.1867 mL 0.3735 mL 0.9336 mL
60 mM 0.0311 mL 0.1556 mL 0.3112 mL 0.7780 mL
80 mM 0.0233 mL 0.1167 mL 0.2334 mL 0.5835 mL
100 mM 0.0187 mL 0.0934 mL 0.1867 mL 0.4668 mL
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  • 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.

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