Roscovitine

Bezeichnung:Roscovitine

CAS-Nr186692-46-6

Englisch Name:Roscovitine

CBNumberCB0367185

SummenformelC19H26N6O

Molgewicht354.45

MOL-Datei186692-46-6.mol

Roscovitine physikalisch-chemischer Eigenschaften

Schmelzpunkt	106～107℃
Siedepunkt	577.5±60.0 °C(Predicted)
Dichte	1.3
storage temp.	-20°C
Löslichkeit	Soluble in DMSO (up to 10 mg/ml, with warming) or in Ethanol (up to 10 mg/ml).
Aggregatzustand	White to off-white solid
pka	14.56±0.10(Predicted)
Farbe	White
Stabilität	Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 3 months.
InChIKey	BTIHMVBBUGXLCJ-OAHLLOKOSA-N
CAS Datenbank	186692-46-6(CAS DataBase Reference)

Sicherheit

S-Sätze:	22-24/25
WGK Germany	3
HS Code	29335990

Gefahreninformationscode (GHS)

Roscovitine Chemische Eigenschaften,Einsatz,Produktion Methoden

S-Sätze Betriebsanweisung:
S22:Staub nicht einatmen.
S24/25:Berührung mit den Augen und der Haut vermeiden.
Beschreibung
Roscovitine (186692-46-6) is a potent and selective inhibitor of cyclin-dependent kinases displaying higher potency and selectivity compared to olomoucine. ?p34 cdc2 IC50 = 0.2 μM.? Also inhibits p33cdk2 and p33cdk5.1? Anti-angiogenic.2 Prevents PPARg S273 phosphorylation, promoting browning of white adipose tissue.3 Enhances peripheral nerve regrowth.4
Verwenden
Roscovitine is a potent and selective inhibitor of cyclin-dependent kinases (CDKs). Roscovitine has been found to produce apoptosis in treated cancerous cells of non-small cell lung cancer (NSCLC) and other cancers. Studies show that Roscovitine displays increased anti-mitotic activity at the G1/S and G2/M phases of the cell cycle. Roscovitine maybe useful in the treatment of non-small cell lung cancer (NSCLC), leukemia, HIV infection, herpes simplex infection, and the mechanisms of chronic inflammation disorders.
Definition
ChEBI: 2,6-Diaminopurine carrying benzylamino, (2R)-1-hydroxybutan-2-yl and isopropyl substituents at C-6, C-2-N and N-9 respectively. It is an experimental drug candidate in the family of pharmacological cyclin-dependent kinase (CDK) inhibitors.
Allgemeine Beschreibung
A potent, reversible, and selective inhibitor of cyclin-dependent kinases (Cdks) that exhibits about ten-fold greater efficacy towards p34^cdk1 and p33^cdk2 and twenty-fold greater efficacy towards p33^cdk5 relative to Olomoucine (Cat. No. 495620). Inhibits p34^cdk1/cyclin B (IC₅₀ = 650 nM), p33^cdk2/cyclin A (IC₅₀ = 700 nM), p33^cdk2/cyclin E (IC₅₀ = 700 nM), and p33^cdk5/p35 (IC₅₀ = 200 nM) by competing for the ATP binding domain of the kinases. Exhibits reduced sensitivity towards related kinases including ERK1 and ERK2 (IC₅₀ = 34 μM and 14 μM, respectively). Roscovitine does not significantly affect the activity of other protein kinases even at 100 μM, including p34^cdk4/cyclin D1 and p40^cdk6/cyclin D2. Compared to olomoucine, roscovitine displays increased anti-mitotic activity at the G₁/S and G₂/M phases of the cell cycle. A 50 mM (5 mg/282 μl) solution of Roscovitine (Cat. No. 557364) in DMSO is also available.
Biochem/physiol Actions
Roscovitine is a purine derived inhibitor. It stimulates apoptosis in cancer cells. It has inhibitory action on mitogen activated protein kinase (MAPK) and M-phase promoting factor (MPF) kinase activity. Roscovitine is known to arrest meiosis and thus, prevent embryonic development.
Anticancer Research
Roscovitine a derivative of olomoucine which is isolated from Raphanus sativus isunder clinical trials (Shoeb 2006).
Lager
Store at -20°C
Einzelnachweise
1) Meijer et al. (1997), Biochemical and cellular effects of roscovitine, a potent and selective inhibitor of the cyclin-dependent kinases cdc2, cdk2 and cdk5 ; Eur. J. Biochem., 243 527 2) Liebl et al. (2011), Anti-angiogenic effects of purine inhibitors of cyclin dependent kinases; Angiogenesis, 14 281 3) Wang et al. (2016) Browning of White Adipose Tissue with Roscovitine Induces a Distinct Population of UCP1+ Adipocytes; Cell Metab. 24 835 4) Law et al. (2016) Enhancement of Peripheral Nerve Regrowth by the Purine Nucleoside Analog and Cell Cycle Inhibitor, Roscovitine; Front. Cell. Neurosci. 10 238

Roscovitine Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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