| Identification | Back Directory | [Name]
KU-0063794 | [CAS]
938440-64-3 | [Synonyms]
CS-28
KU0063794
KU 0063794, >=98%
KU0063794(KU63794)
KU-0063794 USP/EP/BP
KU-0063794(KU 0063794)
mTOR Inhibitor IV, Ku-63794
KU-0063794;KU 0063794; KU0063794
KU-0063794,Etoposide,Etopl,Vepeside.
mTOR Inhibitor IV, Ku-63794 - CAS 938440-64-3 - Calbiochem
(5-(2-((2R,6S)-2,6-Dimethylmorpholino)-4-morpholinopyrido[2,3-d]pyrimidin-7-yl)-2-methoxypheny
BENZENEMETHANOL, 5-[2-[(2R,6S)-2,6-DIMETHYL-4-MORPHOLINYL]-4-(4-MORPHOLINYL)PYRIDO[2,3-D]PYRIMIDIN-7
(5-(2-((2R,6S)-2,6-Dimethylmorpholino)-4-morpholinopyrido[2,3-d]pyrimidin-7-yl)-2-methoxyphenyl)methanol
(5-(2-((2S,6R)-2,6-dimethylmorpholino)-4-morpholinopyrido[2,3-d]pyrimidin-7-yl)-2-methoxyphenyl)methanol
[5-[2-[(2R,6S)-2,6-Dimethylmorpholin-4-yl]-4-morpholino-pyrido[2,3-d]pyrimidin-7-yl]-2-methoxy-phenyl]methanol
5-[2-[(2R,6S)-2,6-Dimethyl-4-morpholinyl]-4-(4-morpholinyl)pyrido[2,3-d]pyrimidin-7-yl]-2-methoxybenzenemethanol
rel-5-[2-[(2R,6S)-2,6-dimethyl-4-morpholinyl]-4-(4-morpholinyl)pyrido[2,3-d]pyrimidin-7-yl]-2-methoxybenzenemethanol
BENZENEMETHANOL, 5-[2-[(2R,6S)-2,6-DIMETHYL-4-MORPHOLINYL]-4-(4-MORPHOLINYL)PYRIDO[2,3-D]PYRIMIDIN-7-YL]-2-METHOXY-, REL-
5-[2-[(2R,6S)-2,6-Dimethyl-4-morpholinyl]-4-(4-morpholinyl)pyrido[2,3-d]pyrimidin-7-yl]-2-methoxybenzenemethanol KU-0063794 | [Molecular Formula]
C25H31N5O4 | [MDL Number]
MFCD11977741 | [MOL File]
938440-64-3.mol | [Molecular Weight]
465.551 |
| Chemical Properties | Back Directory | [Boiling point ]
694.3±65.0 °C(Predicted) | [density ]
1.248 | [storage temp. ]
Store at RT | [solubility ]
DMSO: >2mg/mL (warmed) | [form ]
powder | [pka]
14.20±0.10(Predicted) | [color ]
white to beige | [InChIKey]
RFSMUFRPPYDYRD-CALCHBBNSA-N | [SMILES]
COc1ccc(cc1CO)-c2ccc3c(nc(nc3n2)N4C[C@H](C)O[C@H](C)C4)N5CCOCC5 |
| Hazard Information | Back Directory | [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.1 Ku-0063794 is a cell-permeable, selective dual inhibitor of mTORC1 and mTORC2 (IC50 = 10 nM).2 It does not affect the activity of 76 other protein kinases or seven lipid kinases, including PI3Ks.2 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).2,3,4 | [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)
| [Uses]
Ku 0063794 is a specific mammalian target of rapamycin (mTOR) inhibitor and may be used for the treatment of cancers. | [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 | [References]
[1] JUAN M GARCíA-MARTíNEZ. Ku-0063794 is a specific inhibitor of the mammalian target of rapamycin (mTOR).[J]. Biochemical Journal, 2009, 421 1: 29-42. DOI: 10.1042/bj20090489
[2] SHI-JIANG FEI. Targeting mTOR to overcome epidermal growth factor receptor tyrosine kinase inhibitor resistance in non-small cell lung cancer cells.[J]. PLoS ONE, 2013: e69104. DOI: 10.1371/journal.pone.0069104
[3] HAO ZHANG. A comparison of Ku0063794, a dual mTORC1 and mTORC2 inhibitor, and temsirolimus in preclinical renal cell carcinoma models.[J]. PLoS ONE, 2013: e54918. DOI: 10.1371/journal.pone.0054918 |
|
| Company Name: |
Shangchem Co., Ltd.
|
| Telephone: |
+86-21-68182121 |
| Website: |
www.chemicalbook.com/ShowSupplierProductsList14031/0_EN.htm |
| Company Name: |
NCE Biomedical Co.,Ltd.
|
| Telephone: |
4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988 |
| Website: |
www.chemicalbook.com/ShowSupplierProductsList15748/0_EN.htm |
|