KU-0063794

Bezeichnung:KU-0063794

CAS-Nr938440-64-3

Englisch Name:KU-0063794

CBNumberCB42468008

SummenformelC25H31N5O4

Molgewicht465.54

MOL-Datei938440-64-3.mol

KU-0063794 physikalisch-chemischer Eigenschaften

Siedepunkt	694.3±65.0 °C(Predicted)
Dichte	1.248
storage temp.	2-8°C
Löslichkeit	DMSO: >2mg/mL (warmed)
Aggregatzustand	powder
pka	14.20±0.10(Predicted)
Farbe	white to beige
InChIKey	RFSMUFRPPYDYRD-CALCHBBNSA-N

Sicherheit

Kennzeichnung gefährlicher	T
R-Sätze:	25
S-Sätze:	45
WGK Germany	3

Gefahreninformationscode (GHS)

KU-0063794 Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
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).
Verwenden
Ku 0063794 is a specific mammalian target of rapamycin (mTOR) inhibitor and may be used for the treatment of cancers.
Verwenden
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.
Biologische Aktivität
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).
Lager
Room temperature

KU-0063794 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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