2. PI3K/Akt/mTOR
  3. PI3K mTOR
  4. PI3K/mTOR Inhibitor-11

PI3K/mTOR Inhibitor-11 is an orally active PI3K/mTOR inhibitor (IC50: 3.5, 4.6, and 21.3 nM for PI3Kα, PI3Kδ, and mTOR). PI3K/mTOR Inhibitor-11 regulates the PI3K/AKT/mTOR signaling pathway by inhibiting the phosphorylation of AKT and S6 proteins. PI3K/mTOR Inhibitor-11 can be used in the research of cancers.

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

PI3K/mTOR Inhibitor-11 Chemical Structure

PI3K/mTOR Inhibitor-11 Chemical Structure

CAS No. : 2845104-25-6

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 594 In-stock
Solution
10 mM * 1 mL in DMSO USD 594 In-stock
Solid
5 mg USD 540 In-stock
10 mg USD 850 In-stock
25 mg USD 1750 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

PI3K/mTOR Inhibitor-11 Related Antibodies

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mTOR mTORC1 mTORC2

  • Biological Activity

  • Purity & Documentation

  • References

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Description

PI3K/mTOR Inhibitor-11 is an orally active PI3K/mTOR inhibitor (IC50: 3.5, 4.6, and 21.3 nM for PI3Kα, PI3Kδ, and mTOR). PI3K/mTOR Inhibitor-11 regulates the PI3K/AKT/mTOR signaling pathway by inhibiting the phosphorylation of AKT and S6 proteins. PI3K/mTOR Inhibitor-11 can be used in the research of cancers[1].

IC50 & Target[1]

PI3Kα

3.5 nM (IC50)

PI3Kδ

4.6 nM (IC50)

mTOR

21.3 nM (IC50)

In Vitro

PI3K/mTOR Inhibitor-11 (compound 8o) inhibits various human cancer cell lines HT29, HCT15, H3122, HeLa, SW620, and H446 viability with IC50 values of 0.25, 0.17, 0.29, 0.09, 0.16, and 0.97 μM, respectively[1].
PI3K/mTOR Inhibitor-11 (0-1.25 μM, 15 days) decreases the colony formation rates of HeLa and SW620 cells[1].
PI3K/mTOR Inhibitor-11 (0-2.5 μM, 24 h) arrests HeLa and SW620 cells at the G0/G1 phases[1].
PI3K/mTOR Inhibitor-11 (0-2.5 μM, 24 h) suppressees the phosphorylated AKT and S6 proteins in HeLa cells[1].

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

PI3K/mTOR Inhibitor-11 Related Antibodies

Apoptosis Analysis[1]

Cell Line: HeLa and SW620 cells
Concentration: 0, 0.15625, 0.625, 1.25 μM
Incubation Time: 24 h
Result: Affected HeLa cells’ apoptosis rate from 6.10 to 66.04% in a dose-dependent manner.

Western Blot Analysis[1]

Cell Line: HeLa
Concentration: 0, 0.15625, 0.625, 1.25, 2.5 μM
Incubation Time: 24 h
Result: Suppressed the phosphorylated AKT (Ser473 and Thr308) and S6 proteins.
In Vivo

PI3K/mTOR Inhibitor-11 (compound 8o, 15-60 mg/kg, intragastric administration) suppresses the growth of HeLa and SW620 xenograft tumors[1].
PI3K/mTOR Inhibitor-11 (1 mg/kg for i.v., 10 mg/kg for p.o., rats) shows oral bioavailability (76.81%)[1].

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

Animal Model: HeLa and SW620 xenograft models of female BALB/c nude mice[1].
Dosage: 15, 30, and 60 mg/kg
Administration: Intragastric administration, daily for 30 days.
Result: The TGIs (tumor growth inhibitions): 80.22, 73.50, and 60.79% in the HeLa xenograft model at doses of 60, 30, and 15 mg/kg, respectively.
TGIs: 81.03, 70.81, and 60.58% in the SW620 xenograft model at doses of 60, 30, and 15 mg/kg, respectively.
Animal Model: Rats[1].
Dosage: 1 mg/kg for i.v., 10 mg/kg for p.o.
Administration: i.v., p.o.
Result: Pharmacokinetic parameters of PI3K/mTOR Inhibitor-11 (compound 8o)
dose (mg/kg) T1/2 (h) Cmax (ng/mL) CL (mL/min/kg) F (%)
1 (i.v.) 17.2
10 (p.o.) 2.6 2995 76.81%
Molecular Weight

443.50

Formula

C27H21N7
CAS No.
Appearance

Solid

Color

Off-white to gray

SMILES

CC(C1=NC=C(N2C(C)=NC3=C2C4=CC(C5=CN=C(NC=C6)C6=C5)=CC=C4N=C3)C=C1)(C)C#N
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 : 40 mg/mL (90.19 mM; ultrasonic and warming and heat to 60°C; 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 2.2548 mL 11.2740 mL 22.5479 mL
5 mM 0.4510 mL 2.2548 mL 4.5096 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.

  • Molarity Calculator

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

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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

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: ≥ 4 mg/mL (9.02 mM); Clear solution

    This protocol yields a clear solution of ≥ 4 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 (40.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
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 2.2548 mL 11.2740 mL 22.5479 mL 56.3698 mL
5 mM 0.4510 mL 2.2548 mL 4.5096 mL 11.2740 mL
10 mM 0.2255 mL 1.1274 mL 2.2548 mL 5.6370 mL
15 mM 0.1503 mL 0.7516 mL 1.5032 mL 3.7580 mL
20 mM 0.1127 mL 0.5637 mL 1.1274 mL 2.8185 mL
25 mM 0.0902 mL 0.4510 mL 0.9019 mL 2.2548 mL
30 mM 0.0752 mL 0.3758 mL 0.7516 mL 1.8790 mL
40 mM 0.0564 mL 0.2818 mL 0.5637 mL 1.4092 mL
50 mM 0.0451 mL 0.2255 mL 0.4510 mL 1.1274 mL
60 mM 0.0376 mL 0.1879 mL 0.3758 mL 0.9395 mL
80 mM 0.0282 mL 0.1409 mL 0.2818 mL 0.7046 mL
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PI3K/mTOR Inhibitor-11 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/mTOR Inhibitor-112845104-25-6PI3KmTORPhosphoinositide 3-kinaseMammalian target of RapamycinCancerAKTS6HeLaSW620Inhibitorinhibitorinhibit

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