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| | KU-0063794 Basic information |
| Product Name: | KU-0063794 | | Synonyms: | BENZENEMETHANOL, 5-[2-[(2R,6S)-2,6-DIMETHYL-4-MORPHOLINYL]-4-(4-MORPHOLINYL)PYRIDO[2,3-D]PYRIMIDIN-7-YL]-2-METHOXY-, REL-;KU0063794;5-[2-[(2R,6S)-2,6-Dimethyl-4-morpholinyl]-4-(4-morpholinyl)pyrido[2,3-d]pyrimidin-7-yl]-2-methoxybenzenemethanol;(5-(2-((2R,6S)-2,6-Dimethylmorpholino)-4-morpholinopyrido[2,3-d]pyrimidin-7-yl)-2-methoxyphenyl)methanol;rel-5-[2-[(2R,6S)-2,6-dimethyl-4-morpholinyl]-4-(4-morpholinyl)pyrido[2,3-d]pyrimidin-7-yl]-2-methoxybenzenemethanol;KU0063794(KU63794);KU-0063794(KU 0063794);BENZENEMETHANOL, 5-[2-[(2R,6S)-2,6-DIMETHYL-4-MORPHOLINYL]-4-(4-MORPHOLINYL)PYRIDO[2,3-D]PYRIMIDIN-7 | | CAS: | 938440-64-3 | | MF: | C25H31N5O4 | | MW: | 465.54 | | EINECS: | | | Product Categories: | Inhibitors;Akt;mTOR;PI3K | | Mol File: | 938440-64-3.mol |  |
| | KU-0063794 Chemical Properties |
| Boiling point | 694.3±65.0 °C(Predicted) | | density | 1.248 | | storage temp. | 2-8°C | | solubility | DMSO: >2mg/mL (warmed) | | form | powder | | pka | 14.20±0.10(Predicted) | | color | white to beige | | InChIKey | RFSMUFRPPYDYRD-CALCHBBNSA-N |
| Hazard Codes | T | | Risk Statements | 25 | | Safety Statements | 45 | | WGK Germany | 3 |
| | KU-0063794 Usage And Synthesis |
| Description | The mammalian target of rapamycin (mTOR) is a serine-threonine kinase which acts as part of two distinct complexes, TORC1 and TORC2. Both complexes (TORC1/2) play central roles in cell growth, gene expression, angiogenesis, and cell survival. Ku-0063794 is a cell-permeable, selective dual inhibitor of mTORC1 and mTORC2 (IC50 = 10 nM). It does not affect the activity of 76 other protein kinases or seven lipid kinases, including PI3Ks. Ku-0063794 inhibits cell growth by inducing G1-cell cycle arrest and autophagy, but not apoptosis, and inhibits tumor growth in a xenograft model of renal cell carcinoma (8 mg/kg for 46 days). | | Uses | Ku 0063794 is a specific mammalian target of rapamycin (mTOR) inhibitor and may be used for the treatment of cancers. | | Uses | KU 0063794 has been used:
- as a mammalian target of rapamycin (mTOR) inhibitor to study the effects of follicular stimulating hormone (FSH) in mTOR phosphorylation and vascular cell adhesion molecule-1 (VCAM-1) expression in?human umbilical vascular endothelial cells (HUVECs)
- as a mTOR inhibitor to treat effector memory (EM) CD8+ T cells for metabolic flux analysis
- as an autophagy inducer to demonstrate the utility of p62 and LC3B-II quantification in HEK293T cells and primary cultures of rat neurons and astrocytes using time-resolved fluorescence resonance energy transfer (TR-FRET)
| | Definition | ChEBI: A member of the class of pyridopyrimidines that is an mTOR inhibitor and shows anti-tumour properties. | | Biological Activity | Selective inhibitor of mammalian target of rapamycin (mTOR) (IC 50 ~10 nM for mTORC1 and mTORC2 respectively). Displays no activity at PI 3-kinase or 76 other kinases tested. Inhibits activation and hydrophobic motif phosphorylation of Akt, S6K and SGK, but not RSK. Suppresses cell growth and induces G 1 cell cycle arrest in vitro . | | Biochem/physiol Actions | KU 0063794 induces autophagy. It is cell-permeant and suppresses activation and hydrophobic motif phosphorylation of protein kinase B (Akt), p70 ribosomal S6 kinase (S6K) and serum and glucocorticoid protein kinase (SGK). | | storage | Room temperature |
| | KU-0063794 Preparation Products And Raw materials |
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