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mTOR inhibitor-3

CAS No. : 1207358-59-5

MCE 站：mTOR inhibitor-3

产品活性：mTOR inhibitor-3 是一种有效的 mTOR 抑制剂，K_i 值为 1.5 nM。mTOR inhibitor-3 在细胞实验及体内药代动力学 (PK)/药效学 (PD) 实验中都抑制 mTORC1 和 mTORC2。

研究领域：PI3K/Akt/mTOR

作用靶点：mTOR

In Vitro: mTOR inhibitor-3 (Compound 12i) inhibits mTOR with a K_i of 1.5 nM, 500-fold selectivity over closely related PI3 kinases. mTOR inhibitor-3 inhibits NCI-PC3 and MCF7neo/Her2 cells proliferation with IC₅₀s of 150 nM and 57 nM, respectively.

In Vivo: mTOR inhibitor-3 (Compound 8h) has high free plasma clearance in both mice (1818 mL/min/kg) and rats (1538 mL/min/kg in rat) . mTOR inhibitor-3 (Compounds 12i) is selected for this study due to its potency, selectivity, and favorable mouse PK profile. Plasma levels of mTOR inhibitor-3 6 h following oral administration in PC3 tumor-bearing mice along with the fold decreases of phosphorylated mTORC1 and -2 substrates relative to time-matched vehicle controls. mTOR inhibitor-3 has moderate terminal elimination half-life (t_1/2=1.7 h for mouse(1 mg/kg, iv)). mTOR inhibitor-3 achieves tumor stasis at the highest 200 mg/kg/day dose examined, which appears to also be approaching the limit of tolerability for this molecule.

相关产品：Covalent Screening Library Plus  |  Bioactive Compound Library Plus  |  Kinase Inhibitor Library  |  PI3K/Akt/mTOR Compound Library  |  Stem Cell Signaling Compound Library  |  Anti-Cancer Compound Library  |  Autophagy Compound Library  |  Anti-Aging Compound Library  |  Covalent Screening Library  |  Antioxidants 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  |  Rapamycin  |  Everolimus  |  MHY1485  |  3BDO  |  Temsirolimus  |  Salidroside  |  Torkinib  |  PI-103  |  D-α-Hydroxyglutaric acid disodium  |  L-Leucine  |  Dihydromyricetin  |  PKI-402  |  Polyphyllin I  |  Rheb inhibitor NR1  |  GSK1059615  |  GNE-317  |  PP121  |  WYE-354  |  Cyclovirobuxine D  |  HDACs/mTOR Inhibitor 1  |  XL388  |  ETP-46464  |  Palomid 529  |  WAY-600  |  Arnicolide D  |  (+)-Usnic acid  |  hSMG-1 inhibitor 11j  |  mTOR inhibitor-1  |  TMBIM6 antagonist-1  |  Hederacolchiside A1

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