LY3023414

Catalog No.S8322 Synonyms: GTPL8918

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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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]	+ Expand 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)

References

[1] Smith MC, et al. Mol Cancer Ther. 2016, [Epub ahead of print]

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 Download LY3023414 SDF

Molecular Weight	406.48
Formula	C₂₃H₂₆N₄O₃
CAS No.	1386874-06-1
Storage	3 years -20°C powder
Storage	2 years -80°C in solvent
Synonyms	GTPL8918

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Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2019-03-27)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT03675893	Recruiting	Endometrial Cancer	Dana-Farber Cancer Institute\|Eli Lilly and Company	December 24 2018	Phase 2
NCT03675893	Recruiting	Endometrial Cancer	Dana-Farber Cancer Institute\|Eli Lilly and Company	December 24 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
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
NCT03155620	Recruiting	Advanced Malignant Solid Neoplasm\|Ann Arbor Stage III Childhood Non-Hodgkin Lymphoma\|Ann Arbor Stage IV Childhood Non-Hodgkin Lymphoma\|Childhood Langerhans Cell Histiocytosis\|Histiocytic Sarcoma\|Juvenile Xanthogranuloma\|Malignant Glioma\|Recurrent Central Nervous System Neoplasm\|Recurrent Childhood Ependymoma\|Recurrent Childhood Malignant Germ Cell Tumor\|Recurrent Childhood Medulloblastoma\|Recurrent Childhood Non-Hodgkin Lymphoma\|Recurrent Childhood Rhabdomyosarcoma\|Recurrent Childhood Soft Tissue Sarcoma\|Recurrent Ewing Sarcoma\|Recurrent Glioma\|Recurrent Hepatoblastoma\|Recurrent Langerhans Cell Histiocytosis\|Recurrent Malignant Solid Neoplasm\|Recurrent Neuroblastoma\|Recurrent Osteosarcoma\|Recurrent Peripheral Primitive Neuroectodermal Tumor\|Recurrent Rhabdoid Tumor\|Refractory Central Nervous System Neoplasm\|Refractory Childhood Malignant Germ Cell Tumor\|Refractory Ewing Sarcoma\|Refractory Glioma\|Refractory Hepatoblastoma\|Refractory Langerhans Cell Histiocytosis\|Refractory Malignant Solid Neoplasm\|Refractory Medulloblastoma\|Refractory Neuroblastoma\|Refractory Non-Hodgkin Lymphoma\|Refractory Osteosarcoma\|Refractory Peripheral Primitive Neuroectodermal Tumor\|Refractory Rhabdoid Tumor\|Refractory Rhabdomyosarcoma\|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\|Wilms Tumor	National Cancer Institute (NCI)	July 24 2017	Phase 2
NCT03155620	Recruiting	Advanced Malignant Solid Neoplasm\|Ann Arbor Stage III Childhood Non-Hodgkin Lymphoma\|Ann Arbor Stage IV Childhood Non-Hodgkin Lymphoma\|Childhood Langerhans Cell Histiocytosis\|Histiocytic Sarcoma\|Juvenile Xanthogranuloma\|Malignant Glioma\|Recurrent Central Nervous System Neoplasm\|Recurrent Childhood Ependymoma\|Recurrent Childhood Malignant Germ Cell Tumor\|Recurrent Childhood Medulloblastoma\|Recurrent Childhood Non-Hodgkin Lymphoma\|Recurrent Childhood Rhabdomyosarcoma\|Recurrent Childhood Soft Tissue Sarcoma\|Recurrent Ewing Sarcoma\|Recurrent Glioma\|Recurrent Hepatoblastoma\|Recurrent Langerhans Cell Histiocytosis\|Recurrent Malignant Solid Neoplasm\|Recurrent Neuroblastoma\|Recurrent Osteosarcoma\|Recurrent Peripheral Primitive Neuroectodermal Tumor\|Recurrent Rhabdoid Tumor\|Refractory Central Nervous System Neoplasm\|Refractory Childhood Malignant Germ Cell Tumor\|Refractory Ewing Sarcoma\|Refractory Glioma\|Refractory Hepatoblastoma\|Refractory Langerhans Cell Histiocytosis\|Refractory Malignant Solid Neoplasm\|Refractory Medulloblastoma\|Refractory Neuroblastoma\|Refractory Non-Hodgkin Lymphoma\|Refractory Osteosarcoma\|Refractory Peripheral Primitive Neuroectodermal Tumor\|Refractory Rhabdoid Tumor\|Refractory Rhabdomyosarcoma\|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\|Wilms Tumor	National Cancer Institute (NCI)	July 24 2017	Phase 2

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PI3K Signaling Pathway Map

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LY3023414

1 Customer Review

Purity & Quality Control

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Biological Activity

Protocol

References

Solubility (25°C)

Chemical Information Download LY3023414 SDF

Bio Calculators

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Dilution Calculator

Concentration _(start) x Volume _(start) = Concentration _(final) x Volume _(final)

The Serial Dilution Calculator Equation

Serial Dilutions

Computed Result

Molecular Weight Calculator

Total Molecular Weight: g/mol

Instructions to calculate molar mass (molecular weight) of a chemical compound:

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molarity Calculator

Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2019-03-27)

Tech Support

PI3K Signaling Pathway Map

Related PI3K Products0

Choose Your Country or Region

By Signaling Pathways

By product type

LY3023414

1 Customer Review

Purity & Quality Control

Choose Selective PI3K Inhibitors

Biological Activity

Protocol

References

Solubility (25°C)

Chemical Information Download LY3023414 SDF

Bio Calculators

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Dilution Calculator

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

The Serial Dilution Calculator Equation

Serial Dilutions

Computed Result

Molecular Weight Calculator

Total Molecular Weight: g/mol

Instructions to calculate molar mass (molecular weight) of a chemical compound:

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molarity Calculator

Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2019-03-27)

Tech Support

PI3K Signaling Pathway Map

Related PI3K Products0

Concentration _(start) x Volume _(start) = Concentration _(final) x Volume _(final)