LY3023414

Catalog No.S8322 Synonyms: GTPL8918

LY3023414 Chemical Structure

Molecular Weight(MW): 406.48

LY3023414 is an oral ATP competitive inhibitor of the class I PI3K isoforms, mTOR and DNA-PK.

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  • The structure and formula weight of LY3023414 were presented (A). Established human glioma cells (U251MG and A172 lines), primary human astrocytes (“Astrocytes”) or primary human glioma cells [three lines, “Glioma (L1/2/3)”], were either left untreated (“Ctrl”) or treated with LY3023414 at 1-1000 nM, cells were further cultured for indicated time; Cell survival was tested (B, C, and E) (n=5). Cell proliferation was also tested by the BrdU ELISA assay (D and F) (n=5). *p < 0.05 vs. “Ctrl”. Experiments in this figure were repeated three times.

    Oncotarget, 2017, 8(58): 98964-98973. LY3023414 purchased from Selleck.

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Biological Activity

Description LY3023414 is an oral ATP competitive inhibitor of the class I PI3K isoforms, mTOR and DNA-PK.
Targets
class I PI3K isoforms [1]
()		 mTOR kinase [1]
()		 DNA-PK [1]
()
In vitro

LY3023414 shows high solubility across a wide pH range. In vitro, inhibition of PI3K/AKT/mTOR signaling by LY3023414 causes G1 cell-cycle arrest and resulted in broad antiproliferative activity in cancer cell panel screens. In cell-based assays, LY3023414 inhibition of PI3K and mTOR is assessed in the PTEN-deficient U87 MG glioblastoma cell line. LY3023414 inhibits the phosphorylation of AKT at position T308 downstream of PI3K at an IC50 of 106 nM. Similarly, LY3023414 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 was inhibited as well, indicating target inhibition along the entire PI3K/AKT/mTOR pathway by LY3023414[1].
In vivo In vivo, LY3023414 demonstrates high bioavailability and dose-dependent dephosphorylation of PI3K/AKT/mTOR pathway downstream substrates such as AKT, S6K, S6RP, and 4E-BP1 for 4 to 6 hours, reflecting the drug's half-life of 2 hours. Intermittent target inhibition is sufficient for its antitumor activity. LY3023414 shows time- and dose-dependent target inhibition in vivo. It is currently being evaluated in phase 1 and 2 trials for the treatment of human malignancies[1].

Protocol

Animal Research:

[1]
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  • Animal Models: athymic nude, CD-1 nude and NMRI athymic nude mice(Xenograft tumors)
  • Formulation: 1% HEC in distilled water containing 0.25% polysorbate 80 and 0.05% Dow-Corning Antifoam 1510-US
  • Dosages: --
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro Ethanol 61 mg/mL (150.06 mM)
DMSO 47 mg/mL (115.62 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 406.48
Formula

C23H26N4O3
CAS No. 1386874-06-1
Storage powder
in solvent
Synonyms GTPL8918

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03675893 Not yet recruiting Endometrial Cancer Dana-Farber Cancer Institute|Eli Lilly and Company October 31 2018 Phase 2
NCT03213678 Recruiting Advanced Malignant Solid Neoplasm|Ann Arbor Stage III Non-Hodgkin Lymphoma|Ann Arbor Stage IV Non-Hodgkin Lymphoma|Malignant Glioma|Recurrent Central Nervous System Neoplasm|Recurrent Childhood Ependymoma|Recurrent Ewing Sarcoma|Recurrent Glioma|Recurrent Hepatoblastoma|Recurrent Langerhans Cell Histiocytosis|Recurrent Malignant Germ Cell Tumor|Recurrent Malignant Solid Neoplasm|Recurrent Medulloblastoma|Recurrent Neuroblastoma|Recurrent Non-Hodgkin Lymphoma|Recurrent Osteosarcoma|Recurrent Peripheral Primitive Neuroectodermal Tumor|Recurrent Rhabdomyosarcoma|Recurrent Soft Tissue Sarcoma|Refractory Central Nervous System Neoplasm|Refractory Langerhans Cell Histiocytosis|Refractory Malignant Germ Cell Tumor|Refractory Malignant Solid Neoplasm|Refractory Neuroblastoma|Refractory Non-Hodgkin Lymphoma|Rhabdoid Tumor|Stage III Osteosarcoma AJCC v7|Stage III Soft Tissue Sarcoma AJCC v7|Stage IV Osteosarcoma AJCC v7|Stage IV Soft Tissue Sarcoma AJCC v7|Stage IVA Osteosarcoma AJCC v7|Stage IVB Osteosarcoma AJCC v7|TSC1 Gene Mutation|TSC2 Gene Mutation|Wilms Tumor National Cancer Institute (NCI) July 31 2017 Phase 2
NCT01655225 Recruiting Advanced Cancer|Metastatic Cancer|Non-Hodgkin''s Lymphoma|Metastatic Breast Cancer|Malignant Mesothelioma|Non-small Cell Lung Cancer Eli Lilly and Company July 31 2012 Phase 1
NCT02407054 Recruiting Prostate Cancer Metastatic Eli Lilly and Company|Sarah Cannon Development Innovations April 29 2015 Phase 2
NCT02818335 Completed Healthy Eli Lilly and Company July 2016 Phase 1
NCT02575703 Completed Healthy Eli Lilly and Company October 2015 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID