SNS-032

Bezeichnung:SNS-032

CAS-Nr345627-80-7

Englisch Name:SNS-032

CBNumberCB51518701

SummenformelC17H24N4O2S2

Molgewicht380.53

MOL-Datei345627-80-7.mol

SNS-032 physikalisch-chemischer Eigenschaften

Schmelzpunkt	171-173 °C
Dichte	1.28±0.1 g/cm3(Predicted)
storage temp.	under inert gas (nitrogen or Argon) at 2–8 °C
Löslichkeit	DMSO (Slightly), Methanol (Slightly)
Aggregatzustand	Solid
pka	7.33±0.70(Predicted)
Farbe	White to Off-White

Sicherheit

HS Code

29349990

Gefahreninformationscode (GHS)

SNS-032 Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
Cyclin-dependent kinases (CDKs) are key regulators of cell cycle progression and are therefore promising targets for cancer therapy. SNS-032 is an ATP-competitive inhibitor of Cdk9, 2, and 7 with IC₅₀ values of 4, 38, and 62 nM, respectively. It is selective for these kinases and displays no additional activity against a panel of 190 kinases (IC₅₀s = >1,000 nM). SNS-032 can block the cell cycle, inhibit transcription, and induce apoptosis in multiple myeloma RPMI-8226 cells with an IC₉₀ value of 0.3 μM. This compound has been shown to induce apoptosis by inhibiting the transcription of the anti-apoptotic proteins, Mcl-1 and XIAP.
Chemische Eigenschaften
Off-White Solid
Verwenden
SNS 032 is a selective inhibitor of Cyclin-dependent Kinase (CDK) 2,7, and 9.
Definition
ChEBI: N-(5-{[(5-tert-butyl-1,3-oxazol-2-yl)methyl]sulfanyl}-1,3-thiazol-2-yl)piperidine-4-carboxamide is a secondary carboxamide resulting from the formal condensation of the carboxy group of piperidine-4-carboxylic acid with the amino group of 5-{[(5-tert-butyl-1,3-oxazol-2-yl)methyl]sulfanyl}-1,3-thiazol-2-amine. It is an ATP-competitive inhibitor of CDK2, CDK7 and CDK9 kinases and exhibits anti-cancer properties. It has a role as an apoptosis inducer, an antineoplastic agent, an EC 2.7.11.22 (cyclin-dependent kinase) inhibitor and an angiogenesis inhibitor. It is a piperidinecarboxamide, a member of 1,3-oxazoles, a member of 1,3-thiazoles, an organic sulfide and a secondary carboxamide.
Lager
Store at -20°C
Einzelnachweise
[1]. tong w.g., chen r., plunkett w., et al. phase i and pharmacologic study of sns-032, a potent and selective cdk2, 7, and 9 inhibitor, in patients with advanced chronic lymphocytic leukemia and multiple myeloma. journal of clinical oncology, 2010, 28(18):3015- 3022.
[2]. chipumuro e., marco e., christensen c.l., et al. cdk7 inhibition suppresses super-enhancer-linked oncogenic transcription in mycn-driven cancer. cell, 2014, 159:1-14.
[3]. meng h., jin y.m., liu h., et al. sns-032 inhibits mtorc1/mtorc2 activity in acute myeloid leukemia cells and has synergistic activity with perifosine against akt. journal of hematology & oncology, 2013, 6:18.
[4]. chen r., wierda w.g., chubb s., et al. mechanism of action of sns032, a novel cyclin-dependent kinase inhibitor, in chronic lymphocytic leukemia. blood, 2009, 113(19):4637-4645.

SNS-032 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

345627-80-7, SNS-032 Verwandte Suche:

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