Cat. No.: HY-151622

PI3K/mTOR Inhibitor-11

2 Cited Publications

Customer Review

Based on 2 publication(s) in Google Scholar

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.

Purity: 99.65%
CAS No.: 2845104-25-6
Formula: C₂₇H₂₁N₇
Molecular Weight:443.50

Storage:

4°C, protect from light

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

PI3K/mTOR Inhibitor-11 Chemical Structure

CAS No.: 2845104-25-6

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Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (2)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

PI3Kα

3.5 nM (IC₅₀)

PI3Kδ

4.6 nM (IC₅₀)

mTOR

21.3 nM (IC₅₀)

All PI3K Isoforms :

All mTOR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
HCT-15	IC₅₀	0.17 μM Compound: 8o	Antiproliferative activity against human HCT-15 cells with PIK3CA mutation assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay Antiproliferative activity against human HCT-15 cells with PIK3CA mutation assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay	[PMID: 36191148]
HeLa	IC₅₀	0.09 μM Compound: 8o	Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay	[PMID: 36191148]
HT-29	IC₅₀	0.25 μM Compound: 8o	Antiproliferative activity against human HT-29 cells with PIK3CA mutation assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay Antiproliferative activity against human HT-29 cells with PIK3CA mutation assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay	[PMID: 36191148]
NCI-H3122	IC₅₀	0.29 μM Compound: 8o	Antiproliferative activity against human NCI-H3122 cells assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay Antiproliferative activity against human NCI-H3122 cells assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay	[PMID: 36191148]
NCI-H446	IC₅₀	0.97 μM Compound: 8o	Antiproliferative activity against PTEN-null human NCI-H446 cells assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay Antiproliferative activity against PTEN-null human NCI-H446 cells assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay	[PMID: 36191148]
SW-620	IC₅₀	0.16 μM Compound: 8o	Antiproliferative activity against human SW620 cells assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay Antiproliferative activity against human SW620 cells assessed as inhibition of cell growth incubated for 48 to 72 hrs by MTT assay	[PMID: 36191148]

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.

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) T_1/2 (h) C_max (ng/mL) CL (mL/min/kg) F (%)

1 (i.v.) 17.2

10 (p.o.) 2.6 2995 76.81%

Chemical Information

CAS No. 2845104-25-6
Appearance Solid
Molecular Weight 443.50
Formula C₂₇H₂₁N₇
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)

Publications (2)

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Journal Impact Factor

Int Immunopharmacol

Silencing CXCR6 promotes epithelial-mesenchymal transition and invasion in colorectal cancer by activating the VEGFA/PI3K/AKT/mTOR pathway. [Abstract]

2024 Nov 4;143(Pt 3):113529. PMID: 39500082
Parasit Vectors

Ac-HSP20 regulates autophagy and promotes the encystation of Acanthamoeba castellanii by inhibiting the PI3K/AKT/mTOR signaling pathway. [Abstract]

2024 Aug 19;17(1):347. PMID: 39160562

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)

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

2.2548 mL

11.2740 mL

22.5479 mL

5 mM

0.4510 mL

2.2548 mL

4.5096 mL

10 mM

0.2255 mL

1.1274 mL

2.2548 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 (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

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

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Dilution Calculator

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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 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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
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μL
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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:

%
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (286 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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)
Handling Instructions (2659 KB)

References

[1]. Yang J, et al. Discovery of 2-Methyl-2-(4-(2-methyl-8-(1H-pyrrolo[2,3-b]pyridin-6-yl)-1H-naphtho[1,2-d]imidazol-1-yl)phenyl)propanenitrile as a Novel PI3K/mTOR Inhibitor with Enhanced Antitumor Efficacy In Vitro and In Vivo. J Med Chem. 2022 Oct 13;65(19):12781-12801. [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

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

Keywords

PI3K/mTOR Inhibitor-11

2 Cited Publications

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dose (mg/kg)	T_1/2 (h)	C_max (ng/mL)	CL (mL/min/kg)	F (%)
1 (i.v.)			17.2
10 (p.o.)	2.6	2995		76.81%

PI3K/mTOR Inhibitor-11

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Kinase Inhibitor Library

PI3K/Akt/mTOR Compound Library

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Publications Citing Use of MedChemExpress (MCE) PI3K/mTOR Inhibitor-11

All PI3K Isoforms

All mTOR Isoforms

Biological Activity

Chemical Information

Publications (2)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

PI3K/mTOR Inhibitor-11 Related Classifications

HY-151622 Related Classifications