PI3K/mTOR Inhibitor-1

Modify Date: 2024-01-11 21:16:49

PI3K/mTOR Inhibitor-1 Structure
PI3K/mTOR Inhibitor-1 structure
Common Name PI3K/mTOR Inhibitor-1
CAS Number 1949802-49-6 Molecular Weight 407.46
Density N/A Boiling Point N/A
Molecular Formula C18H22FN5O3S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of PI3K/mTOR Inhibitor-1


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[1]. Antitumor activity[1].

 Names

Name PI3K/mTOR Inhibitor-1

 PI3K/mTOR Inhibitor-1 Biological Activity

Description 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[1]. Antitumor activity[1].
Related Catalog
Target

PI3Kα:20 nM (IC50)

PI3Kβ:376 nM (IC50)

PI3Kγ:204 nM (IC50)

PI3Kδ:46 nM (IC50)

mTOR:186 nM (IC50)

In Vitro PI3K/mTOR Inhibitor-1 (Compound 26) also exhibits potent functional suppression of AKT phosphorylation (IC50=196 nM), and excellent antiproliferative effects on a panel of cancer cells[1]. PI3K/mTOR Inhibitor-1 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].
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].
References

[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.

 Chemical & Physical Properties

Molecular Formula C18H22FN5O3S
Molecular Weight 407.46