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Samotolisib

CAS No. : 1386874-06-1

MCE 站：Samotolisib

产品活性：Samotolisib (LY3023414) 有效且选择性地抑制 PI3Kα，PI3Kβ，PI3Kδ，PI3Kγ，DNA-PK，和 mTOR ，IC₅₀ 分别为 6.07 nM，77.6 nM，38 nM，23.8 nM，4.24 nM，和 165 nM。在低纳摩尔浓度下，Samotolisib 有效抑制 mTORC1/2。

研究领域：PI3K/Akt/mTOR  |  Cell Cycle/DNA Damage  |  Autophagy

作用靶点：PI3K  |  DNA-PK  |  mTOR  |  Autophagy

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.

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. Of note, the total daily dose of Samotolisib appears to result in equipotent antitumor activity: 12 mg/kg once daily and 6 mg/kg twice daily produces similar delta T/C values (42% and 38%, respectively) in U87 MG.

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