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Formula | C21H22N6O3 |
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Molecular Weight | 406.44 | CAS No. | 936890-98-1 | |
Solubility (25°C)* | In vitro | DMSO | 81 mg/mL (199.29 mM) | |
Water | Insoluble | |||
Ethanol | Insoluble | |||
* <1 mg/ml means slightly soluble or 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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | OSI-027 (ASP4786, CERC 006, AEVI-006) is a selective and potent dual inhibitor of mTORC1 and mTORC2 with IC50 of 22 nM and 65 nM in cell-free assays, and more than 100-fold selectivity observed for mTOR than PI3Kα, PI3Kβ, PI3Kγ or DNA-PK. OSI-027 induces autophagy in cancer cells. | ||||||||
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In vitro | OSI-027 shows the selective and ATP competitive inhibition activities against mTORC1 and mTORC2 with IC50 of 22 nM and 65 nM, respectively. In addition, OSI-027 inhibits mTOR signaling of phospho-4E-BP1 with an IC50 of 1 μM in cell-based assays. [1] OSI-027 exhibits anti-proliferative activities against several acute leukemia cell lines of myeloid/megakaryocytic origin in a dose-dependent manner, including U937, KG-1, KBM-3B, ML-1, HL-60, and MEG-01 cells. [2] A recent study shows that inhibition of mTORC1/2 by OSI-027 effectively suppresses phosphorylation of Akt (S473) and cell proliferation in breast cancer cells. [3] |
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In vivo | In GEO colorectal xenograft, OSI-027 (65 mg/kg) inhibits both mTORC1 and mTORC2 effectors, including 4E-BP1, Akt, and S6 phosphorylation. Furthermore, mTORC1 and mTORC2 inhibition together by OSI-027 potently inhibits tumor growth more than mTORC1 inhibition by rapamycin. [1] |
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Data from [Urol Oncol, 2013, 1078-1439(13)00251-2]
Data from [Data independently produced by , , Br J Cancer, 2016, 114(6):650-8]
Data from [Data independently produced by , , Cell Physiol Biochem, 2018, 46(2):676-686]
Data from [Data independently produced by , , Sci Rep, 2016, 6:28945]
Three generations of mTOR kinase inhibitors in the activation of the apoptosis process in melanoma cells [ J Cell Commun Signal, 2023, 17(3):975-989] | PubMed: 37097377 |
hnRNP C modulates MERS-CoV and SARS-CoV-2 replication by governing the expression of a subset of circRNAs and cognitive mRNAs [ Emerg Microbes Infect, 2022, 11(1):519-531] | PubMed: 35060842 |
Combined inhibition of BET bromodomain and mTORC1/2 provides therapeutic advantage for rhabdomyosarcoma by switching cell death mechanism [ Mol Carcinog, 2022, 10.1002/mc.23414] | PubMed: 35472745 |
Minimal mitochondrial respiration is required to prevent cell death by inhibition of mTOR signaling in CoQ-deficient cells [ Cell Death Discov, 2021, 7(1):201] | PubMed: 34349107 |
Dual Inhibition of mTORC1/2 Reduces Migration of Cholangiocarcinoma Cells by Regulation of Matrixmetalloproteinases [ Front Cell Dev Biol, 2021, 9:785979] | PubMed: 35096817 |
Mitochondrial Genome-Derived circRNA mc-COX2 Functions as an Oncogene in Chronic Lymphocytic Leukemia [ Mol Ther Nucleic Acids, 2020, 1;20:801-811] | PubMed: 32438315 |
Combined mTORC1/mTORC2 inhibition blocks growth and induces catastrophic macropinocytosis in cancer cells. [ Proc Natl Acad Sci U S A, 2019, 10.1073/pnas.1911393116] | PubMed: 31732667 |
Reverting chemoresistance of targeted agents by a ultrasoluble dendritic nanocapsule. [ J Control Release, 2019, 317:67-77] | PubMed: 31756395 |
Targeting mTOR suppressed colon cancer growth through 4EBP1/eIF4E/PUMA pathway. [ Cancer Gene Ther, 2019, 10.1038/s41417-019-0117-7] | PubMed: 31257364 |
Targeting mTORC1/2 with OSI-027 inhibits proliferation and migration of keloid keratinocytes [ Exp Dermatol, 2019, 28(3):270-275] | PubMed: 30650200 |
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