country

Change Language

EN - English
FR - Français
DE - Deutsch
ES - Español
JA - 日本語
KO - 한국어

Country or Region:

United States

Product Name	Size / Unit Price	Qty

Total: USD 0.00 Checkout

Art. -Nr.: HY-112602

Copy Link Print Information

PI3K/mTOR Inhibitor-1

1 Cited Publications

Kundenbewertung

Based on 1 publication(s) in Google Scholar

PI3K/mTOR Inhibitor-1 is a potent, orally bioavailable dual PI3K/mTOR inhibitor with IC₅₀s of 20/376/204/46 nM and 186 nM for PI3Kα/PI3Kβ/PI3Kγ/PI3Kδ and mTOR, respectively. Antitumor activity.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

CAS. Nr.: 1949802-49-6
Formel: C₁₈H₂₂FN₅O₃S
Molecular Weight:407.46

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (276 KB)

PI3K/mTOR Inhibitor-1 Chemical Structure

CAS. Nr.: 1949802-49-6

Größe

Preis

Verfügbarkeit

Menge

Amount: USD 0.00

* Bitte wählen Sie Menge, bevor Sie Artikel hinzufügen.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

PI3Kα

20 nM (IC₅₀)

PI3Kβ

376 nM (IC₅₀)

PI3Kγ

204 nM (IC₅₀)

PI3Kδ

46 nM (IC₅₀)

mTOR

186 nM (IC₅₀)

Alle PI3K Isoform-spezifische Produkte anzeigen :

Alle mTOR Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HUVEC	IC₅₀	0.108 μM Compound: 26	Cytotoxicity against HUVEC after 72 hrs by MTT assay Cytotoxicity against HUVEC after 72 hrs by MTT assay	[PMID: 30034607]
MCF7	IC₅₀	0.011 μM Compound: 26	Antiproliferative activity against human MCF7 cells harboring PIK3CA E545K mutant after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells harboring PIK3CA E545K mutant after 72 hrs by MTT assay	[PMID: 30034607]
T47D	IC₅₀	0.03 μM Compound: 26	Antiproliferative activity against human T47D cells harboring PI3KCA H1047R mutant after 72 hrs by MTT assay Antiproliferative activity against human T47D cells harboring PI3KCA H1047R mutant after 72 hrs by MTT assay	[PMID: 30034607]

In Vitro

PI3K/mTOR Inhibitor-1 (Compound 26) also exhibits potent functional suppression of AKT phosphorylation (IC₅₀=196 nM)^[1].
PI3K/mTOR Inhibitor-1 (0.046-10 µM, 72 hours) exhibits excellent antiproliferative effects on a panel of cancer cells. PI3K/mTOR Inhibitor inhibits A431, A549, PC3, MDA-MB-361, SW480, ES-2, HT29, SK-OV-3, HCT116 , G401 , BT20 ,DLD1 HCC827, H1650, H460, Farage, H820, HCT15, H358, Colo-205, PC9, H1975, WSU-DLCL2, HT, A2780, SU-DHL-10, Toledo,SU-DHL-6, DB, and Pfeiffer cells with IC₅₀s of 0.188, 0.104, 0.063, 0.085, 0.534, 0.179, 0.163, 0.135, 0.308, 0.113, 0.729, 0.264, 0.287, 1.662, 0.611, 0.202, 0.365, 0.104, 0.098, 0.109, 0.237, 0.136, 0.145, 0.090, 0.251 0.215, 0.269, 0.111 0.062, and 0.061 µM, respectively^[1].

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

Cell Proliferation Assay^[1]

Cell Line:

U87-MG, A431, MCF-7, PC3, A549, MDA-MB-361, SW480, ES-2, HT29, SK-OV-3, HCT116, G401, BT20, DLD1, HCC827, H1650, H460, Farage, H820, HCT15, H358, Colo-205, PC9, H1975, WSU-DLCL2, HT, A2780, SU-DHL-10, Toledo, SU-DHL-6, DB, Pfeiffer cells
Concentration:

0.046-10 µM
Incubation Time:

72 hours
Result:

Inhibited HT-29 cells proliferation with an IC₅₀ of 0.163 μM.

In Vivo

PI3K/mTOR Inhibitor-1 (Compound 26) produces 54.4% tumor growth inhibition (TGI) with daily oral doses of 3.75 mg/kg for 27 days. The 7.5 mg/kg group of PI3K/mTOR Inhibitor-1 displays more significant TGI (72.9%). All animals survive after 27-day treatment, whereas 15% weigh loss is observed in PI3K/mTOR Inhibitor-1, 7.5 mg/kg group^[1].

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

Animal Model:

Balb/c nu/nu mice with HT-29 colorectal carcinoma xenograft mouse model carrying the PIK3CA P449T mutation^[1]
Dosage:

3.75 and 7.5 mg/kg
Administration:

Oral gavage daily for 27 days
Result:

Tumor growth inhibition (TGI) was 54.4% and 72.9% for daily oral doses of 3.75 mg/kg and 7.5 mg/kg for 27 days, respectively.

Chemical Information

CAS. Nr. 1949802-49-6
Molecular Weight 407.46
Formel C₁₈H₂₂FN₅O₃S
SMILES

NC1=CC(F)=C(C2=CC(C3(CC3)S(=O)(C)=O)=NC(N4[C@@H](C)COCC4)=N2)C=N1
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Publications (1)

All

Sort by:

Journal Impact Factor

Environ Pollut

BPA modulates the WDR5/TET2 complex to regulate ERβ expression in eutopic endometrium and drives the development of endometriosis. [Abstract]

2021 Jan 1;268(Pt B):115748. PMID: 33022573

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 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)

Verweise

[1]. Shen S, et al. Discovery of an Orally Bioavailable Dual PI3K/mTOR Inhibitor Based on Sulfonyl-Substituted Morpholinopyrimidines. ACS Med Chem Lett. 2018 Jun 25;9(7):719-724. [Content Brief]

Calculators

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)}

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.

Keywords

PI3K/mTOR Inhibitor-1

1 Cited Publications

100 mg Angebot einholen

Subscribe to the

MedChemExpress

Newsletter

MOQ

Minimum order quantity

100 mg

Angebot einholen Auf Lager

Other size

Angebot einholen

Amount: USD 0.00

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Reinheit & Dokumentation
Verweise

Produktname:
Art. -Nr.:
Menge:
MCE Japan Authorized Agent:

Produktname:
CAS. Nr.:
Species:
Reinheit:
Menge:

PI3K/mTOR Inhibitor-1

Publications Citing Use of MedChemExpress (MCE) PI3K/mTOR Inhibitor-1

Alle PI3K Isoform-spezifische Produkte anzeigen

Alle mTOR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

PI3K/mTOR Inhibitor-1 Related Classifications

HY-112602 Related Classifications