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CAS No. : 1386874-06-1
MCE 国际站: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.
相关产品:Drug Repurposing Compound Library Plus | Clinical Compound Library Plus | Bioactive Compound Library Plus | Cell Cycle/DNA Damage Compound Library | Kinase Inhibitor Library | PI3K/Akt/mTOR Compound Library | Stem Cell Signaling Compound Library | Anti-Cancer Compound Library | Clinical Compound Library | Autophagy Compound Library | Anti-Aging Compound Library | Drug Repurposing Compound Library | Antioxidant Compound Library | Differentiation Inducing Compound Library | Reprogramming Compound Library | Oxygen Sensing Compound Library | Glycolysis Compound Library | Cytoskeleton Compound Library | Glutamine Metabolism Compound Library | Anti-Breast Cancer Compound Library | Anti-Lung Cancer Compound Library | Anti-Pancreatic Cancer Compound Library | Anti-Blood Cancer Compound Library | Anti-Cancer Metabolism Compound Library | Anti-Obesity Compound Library | Angiogenesis-Related Compound Library | Lipid Metabolism Compound Library | Glucose Metabolism Compound Library | Anti-Liver Cancer Compound Library | Anti-Colorectal Cancer Compound Library | Anti-Prostate Cancer Compound Library | Anti-Pulmonary Fibrosis Compound Library | Cancer Stem Cells Compound Library | Pain-Related Compound Library | Mitochondrial Protection Compound Library | Membrane Protein-targeted Compound Library | Highly Selective Inhibitors Library | Highly Selective Activators Library | D-α-Hydroxyglutaric acid disodium | Umbralisib hydrochloride | PI3K-IN-22 | Rigosertib sodium | PI3Kδ/γ-IN-2 | DNA-PK-IN-1 | PI3kδ inhibitor 1 | WYE-354 | GSK2292767 | PI3K-IN-28 | PI3K/mTOR Inhibitor-13 | Disitertide diammonium | 1,3-Dicaffeoylquinic acid | Palomid 529 | Quercetin dihydrate | DNA-PK-IN-3 | PI3Kγ inhibitor 4 | PI-103 Hydrochloride | Hirsutenone | SN32976 | (+)-Usnic acid | Sophocarpine monohydrate | Heterophyllin B | IC-87114 | Phosphatidylinositol 4,5-bisphosphate | Chaetominine | SF2523 | Flupentixol | 8-Aminoadenosine | GNE-490
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货号: HY-12513
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