2. PI3K/Akt/mTOR
  3. mTOR PI3K
  4. PI3K/mTOR-IN-20

PI3K/mTOR-IN-20 is a selective dual PI3K/mTOR inhibitor. PI3K/mTOR-IN-20 demonstrates nanomolar antiproliferative effects with IC50s of 0.380 and 0.090 μM for MRC-5 and Mlg2908 cells. PI3K/mTOR-IN-20 reduces Ashcroft scores, hydroxyproline content, collagen deposition, and downregulates fibrosis-related proteins, while restoring lung architecture in a Bleomycin-induced pulmonary fibrosis model. PI3K/mTOR-IN-20 shows a favorable safety profile with steady weight recovery and no distinct liver or kidney toxicity. PI3K/mTOR-IN-20 can be used for fetal lung fibroblasts research.

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

PI3K/mTOR-IN-20

PI3K/mTOR-IN-20 Chemical Structure

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

PI3K/mTOR-IN-20 Related Antibodies

Top Publications Citing Use of Products

View All mTOR Isoform Specific Products:

View All Isoforms
mTOR mTORC1 mTORC2

View All PI3K Isoform Specific Products:

View All Isoforms
PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

PI3K/mTOR-IN-20 is a selective dual PI3K/mTOR inhibitor. PI3K/mTOR-IN-20 demonstrates nanomolar antiproliferative effects with IC50s of 0.380 and 0.090 μM for MRC-5 and Mlg2908 cells. PI3K/mTOR-IN-20 reduces Ashcroft scores, hydroxyproline content, collagen deposition, and downregulates fibrosis-related proteins, while restoring lung architecture in a Bleomycin-induced pulmonary fibrosis model. PI3K/mTOR-IN-20 shows a favorable safety profile with steady weight recovery and no distinct liver or kidney toxicity. PI3K/mTOR-IN-20 can be used for fetal lung fibroblasts research[1].
IC50 & Target[1].

PI3Kα

 

PI3Kβ

 

PI3Kγ

 

PI3Kδ

 

PI3K

 

In Vitro

PI3K/mTOR-IN-20 (compound 11) (72 h) exhibits nanomolar antiproliferative activity against MRC-5 and Mlg2908 cells with IC50 = 0.38 and 0.09 μM respectively[1].
PI3K/mTOR-IN-20 (1 μM) effectively inhibits highly mTOR and and class I PI3K isoforms (α, β, and y) while exhibiting weaker activity against Pl3k (inhibition rate = 94.89, 79.24, 42.60 and 42.99 % for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ and mTOR respectively[1].
PI3K/mTOR-IN-20 (1 μM, 48h) effectively inhibits PI3K activity and attenuates fibroblast activation in MRC-5 cells[1].

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

PI3K/mTOR-IN-20 Related Antibodies

Western Blot Analysis[1]

Cell Line: MRC-5 cells
Concentration: 1 μM
Incubation Time: 48h
Result: Significantly reduced AKT phosphorylation (pAKT).
Suppressed the expression of key pulmonary fibrosis-associated proteins, fibroblast activation protein (FAP), fibronectin (FN), and α-smooth muscle actin (α-SMA).
Parmacokinetics
Species Dose Route T1/2 Cmax AUC0-∞ F CL Vss
Mice[1] 2.5 mg/kg i.p. 0.79 h 449 ng/mL 315 ng·h/mL 109 % / /
Mice[1] 2.5 mg/kg i.v. 1.11 h / 290 h·ng/g / 150 mL/min/kg 3.7 L/kg
In Vivo

PI3K/mTOR-IN-20 (compound 11) (15 mg/kg, ip, daily for 11 days) exerts robust antifibrotic effects, mitigating collagen deposition, restoring lung architecture, suppressing profibrotic and improving physiological outcomes with safety profile in a Bleomycin (BLM) induced pulmonary fibrosis mice model[1].
PI3K/mTOR-IN-20 (15-60 mg/kg, i.p., once daily for 3 days) exhibits no appreciable liver or kidney toxicity in a bleomycin (BLM) induced pulmonary fibrosis mice model[1].

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

Animal Model: Bleomycin (HY-108345A) (0.75 U/kg, i.p.) induced-male C57BL/6 mice (8-10 weeks)[1]
Dosage: 15 mg/kg
Administration: i.p., daily for 11 days
Result: Significantly attenuated the pathological changes, partially restoring normal lung structure and extensiving fibrotic remodeling[1].
Reduced Ashcroft scores, a quantitative measure of fibrosis severity[1].
Reversed the BLM-induced increase in the lung index (lung-to-body weight ratio), which reflects edema and fibrotic mass accumulation[1].
Robustly suppressed BLM-induced increase in d collagen deposition (a hallmark of fibrosis progression) [1].
Mitigated BLM-induced weight loss and maintained steady weight recovery[1].
Significantly inhibited fibroblast activation protein (FAP) expression[1].
Animal Model: ICR mice (8 weeks)[1]
Dosage: 15, 30, or 60 mg/kg
Administration: i.p., once daily for 3 days
Result: Revealed minimal toxicity in liver and kidney function[1].
Remained Serum levels of alanine transaminase (ALT) and aspartate transaminase (AST) within the normal range at doses of 15 and 30 mg/kg[1].
Unchanged serum creatinine (CREA) and uric acid (UA) levels (markers of kidney function) [1].
No Obvious structure changes occur in the livers[1].
Molecular Weight

618.61

Formula

C29H24F2N8O4S
SMILES

COC1=C(C=C(C2=NN3C(C=C2)=NC=C3C4=CN(N=N4)CCCC5=CC=C(C=C5)O)C=N1)NS(=O)(C6=CC=C(C=C6F)F)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

PI3K/mTOR-IN-20 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
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-IN-20mTORPI3KMammalian target of RapamycinPhosphoinositide 3-kinaseAshcroft scoresfetal lung fibroblastsInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
PI3K/mTOR-IN-20
Cat. No.:
HY-180556
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.