8-[5-(1-hydroxy-1-methylethyl)pyridin-3-yl]-1-[(2S)-2-methoxypropyl]-3-methyl-1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-one
LY3023414
CAS: 1386874-06-1
Molecular Formula: C23H26N4O3
8-[5-(1-hydroxy-1-methylethyl)pyridin-3-yl]-1-[(2S)-2-methoxypropyl]-3-methyl-1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-one - Names and Identifiers
8-[5-(1-hydroxy-1-methylethyl)pyridin-3-yl]-1-[(2S)-2-methoxypropyl]-3-methyl-1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-one - Physico-chemical Properties
| Molecular Formula | C23H26N4O3 |
| Molar Mass | 406.48 |
| Density | 1.239±0.06 g/cm3(Predicted) |
| Boling Point | 591.7±50.0 °C(Predicted) |
| Solubility | 10 mM in DMSO |
| pKa | 13.65±0.29(Predicted) |
| Storage Condition | -20℃ |
| In vitro study | In Vitro, LY3023414 caused cell cycle G1 phase arrest by inhibiting PI3K/AKT/mTOR, resulting in significant anti-proliferative activity in cancer cells. In cell experiments, the inhibitory effect of LY3023414 on PI3K and mTOR was detected in U87 MG glioma cell line with PTEN deficiency. LY3023414 inhibits phosphorylation of AKT(T308) with an IC50 of 106 nM. Similarly, LY3023414 inhibits phosphorylation of AKT(S473) by mTORC2 (IC50=94.2 nM) and mTORC1 kinase targets p70S6K(T389) and 4E-BP1(T37/46) phosphorylation (IC50 10.6 nM and 187 nM, respectively). LY3023414 inhibits the phosphorylation of downstream S6RP(pS240/244) by p70S6K, indicating that LY3023414 can inhibit the entire PI3K/AKT/mTOR signaling pathway target. |
| In vivo study | In Vivo, LY3023414 has high bioavailability and dephosphorylates downstream substrates such as AKT, S6K, S6RP and 4E-BP1 in the PI3K/AKT/mTOR pathway in a dose-dependent manner, its in vivo half-life is 2 hours. Intermittent target inhibition can make LY3023414 fully exert anti-tumor activity. The inhibitory effect of LY3023414 in vivo was time-and concentration-dependent. It is currently in Phase1 and Phase2 clinical trials for the treatment of human malignancies. |
8-[5-(1-hydroxy-1-methylethyl)pyridin-3-yl]-1-[(2S)-2-methoxypropyl]-3-methyl-1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-one - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.46 ml | 12.301 ml | 24.602 ml |
| 5 mM | 0.492 ml | 2.46 ml | 4.92 ml |
| 10 mM | 0.246 ml | 1.23 ml | 2.46 ml |
| 5 mM | 0.049 ml | 0.246 ml | 0.492 ml |
Last Update：2024-01-02 23:10:35
8-[5-(1-hydroxy-1-methylethyl)pyridin-3-yl]-1-[(2S)-2-methoxypropyl]-3-methyl-1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-one - Reference Information
| biological activity | LY3023414 (Samotolisib, GTPL8918) is an oral ATP competitive inhibitor that inhibits Class I PI3K subtypes, mTOR and DNA-PK. |
| Target | Value |
Last Update：2024-04-09 20:52:54
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Product Name: LY3023414 Visit Supplier Webpage Request for quotation
CAS: 1386874-06-1
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
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CAS: 1386874-06-1
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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