Art. -Nr.: HY-12513

Samotolisib

(Synonyms: LY3023414)

8 Cited Publications

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Based on 8 publication(s) in Google Scholar

Samotolisib (LY3023414) potently and selectively inhibits class I PI3K isoforms, DNA-PK, and mTORC1/2 with IC₅₀s of 6.07 nM, 77.6 nM, 38 nM, 23.8 nM, 4.24 nM and 165 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ, DNA-PK and mTOR, respectively. Samotolisib potently inhibits mTORC1/2 at low nanomolar concentrations.

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Reinheit: 98.85%
CAS. Nr.: 1386874-06-1
Formel: C₂₃H₂₆N₄O₃
Molecular Weight:406.48

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Samotolisib Chemical Structure

CAS. Nr.: 1386874-06-1

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (8)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[2]

PI3Kα

6.07 nM (IC₅₀)

PI3Kγ

23.8 nM (IC₅₀)

PI3Kδ

38 nM (IC₅₀)

PI3Kβ

77.6 nM (IC₅₀)

DNA-PK

4.24 nM (IC₅₀)

mTOR

165 nM (IC₅₀)

mTORC1

mTORC2

Alle PI3K Isoform-spezifische Produkte anzeigen :

Alle mTOR Isoform-spezifische Produkte anzeigen :

In Vitro

In cell-based assays, Samotolisib (LY3023414) inhibition of PI3K and mTOR is assessed in the PTEN-deficient U87 MG glioblastoma cell line. Samotolisib inhibits the phosphorylation of Akt at position T308 downstream of PI3K at an IC₅₀ of 106 nM. Similarly, Samotolisib inhibits phosphorylation of Akt at position S473 (IC₅₀=94.2 nM) by mTORC2 as well as phosphorylation of mTORC1 kinase targets p70S6K (position T389; IC₅₀=10.6 nM) and 4E-BP1 (positions T37/46; IC₅₀=187 nM). The downstream phosphorylation of S6RP at positions pS240/244 (IC₅₀=19.1 nM) by p70S6K is inhibited as well, indicating target inhibition along the entire PI3K/Akt/mTOR pathway by Samotolisib. Similar IC₅₀ concentrations for PI3K and mTOR phosphorylation targets are observed in other cell lines with activated PI3K/Akt/mTOR pathways. The ability of Samotolisib to inhibit cancer cell proliferation is evaluated in 32 human cancer cell lines from different tumor types in culture after Samotolisib treatment for 2 to 3 cell doublings in dose–response studies. Samotolisib demonstrates potent single-agent activity and IC₅₀ values below 122 nM in half of the cell lines tested^[1].

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

In Vivo

The ability of Samotolisib (LY3023414) to inhibit tumor growth is studied in several xenograft models exhibiting mutations or deletions that activate the PI3K/Akt/mTOR pathway. Treatment with Samotolisib at 3, 6, or 10 mg/kg twice daily orally for 28 days results in dose-responsive inhibition of tumor growth in the PTEN-deleted U87 MG xenograft model. This treatment produces similar TGI in models exhibiting PTEN truncation (786-O), activating PI3Kα mutation (NCI-H1975), and transgenic Eμ-myc mutant PI3Kα-driven leukemia models^[1].

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 1386874-06-1
Appearance Solid
Molecular Weight 406.48
Formel C₂₃H₂₆N₄O₃
Color Light yellow to yellow
SMILES

O=C(N1C[C@@H](OC)C)N(C)C2=C1C3=CC(C4=CC(C(C)(O)C)=CN=C4)=CC=C3N=C2
Synonyms

LY3023414
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (8)

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Journal Impact Factor

Oncogene

Jumonji histone demethylases are therapeutic targets in small cell lung cancer. [Abstract]

2024 Sep;43(38):2885-2899. PMID: 39154123
Front Pharmacol

CC-223, NSC781406, and BGT226 Exerts a Cytotoxic Effect Against Pancreatic Cancer Cells via mTOR Signaling. [Abstract]

2020 Nov 11;11:580407. PMID: 33343350
Gynecol Oncol

Synergistic effects of a combined treatment of PI3K/mTOR dual inhibitor LY3023414 and carboplatin on human endometrial carcinoma. [Abstract]

2021 Sep;162(3):788-796. PMID: 34183163
Toxicol Appl Pharmacol

In silico and in vitro assessment of drugs potentially causing adverse effects by inhibiting CYP17A1. [Abstract]

2024 May:486:116945. PMID: 38688424
Arch Pharm (Weinheim)

Discovery of potent CSK inhibitors through integrated virtual screening and molecular dynamic simulation. [Abstract]

2024 Sep;357(9):e2400066. PMID: 38809025
PLoS One

Efficacy of NAMPT inhibition in T-cell acute lymphoblastic leukemia. [Abstract]

2025 Jun 17;20(6):e0324443. PMID: 40526635
J Surg Res

Anal Cancer Prevention Through the Topical Use of Single or Dual PI3K/mTOR Inhibitors. [Abstract]

2023 Feb:282:137-146. PMID: 36274448
J Cancer Sci Clin Ther

Systemic Delivery of a Dual PI3K/mTOR Inhibitor More Effective than Topical Delivery in Preventing Anal Carcinogenesis in an HPV Transgenic Mouse Model. [Abstract]

2022;6(2):157-173. PMID: 36683775

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 50 mg/mL (123.01 mM; Need ultrasonic; 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

2.4601 mL

12.3007 mL

24.6015 mL

5 mM

0.4920 mL

2.4601 mL

4.9203 mL

10 mM

0.2460 mL

1.2301 mL

2.4601 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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 40% PEG300 5% Tween-80 45% Saline