ZSTK474

Bezeichnung:ZSTK474

CAS-Nr475110-96-4

Englisch Name:ZSTK474

CBNumberCB0505419

SummenformelC19H21F2N7O2

Molgewicht417.41

MOL-Datei475110-96-4.mol

ZSTK474 physikalisch-chemischer Eigenschaften

Schmelzpunkt	217-219 °C(Solv: ethanol (64-17-5))
Siedepunkt	640.3±65.0 °C(Predicted)
Dichte	1.57
storage temp.	-20°C
Löslichkeit	Soluble in DMSO (up to 20 mg/ml) or in Ethanol (up to 2.5 mg/ml with warming).
Aggregatzustand	White powder.
pka	5.21±0.10(Predicted)
Farbe	White or off-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.

Sicherheit

HS Code

29349990

ZSTK474 Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
ZSTK474 (475110-96-4) is a novel Class I phosphatidylinositol 3-kinase (PI3K) inhibitor. ZSTK474 is an ATP-competitive inhibitor of all four Class I PI3K isoforms. However, it inhibits PI3Kδ most potently, with a Ki of 1.8 nM, while inhibiting the α, β and γ isoforms at slightly higher concentrations (6.7 nM, 10.4 nM and 11.7 nM, respectively)1. Displays potent antitumor activity against human cancer xenografts (A549, PC-3 and WiDr) when administered to mice2. ZSTK474 displays potent anti-inflammatory activity via modulation of human CD14+ monocyte-derived dendritic cell functions and suppresses experimental autoimmune encephalomyelitis3. Ameliorates the progression of adjuvant-induced arthritis in a rat model4.
Verwenden
ZSTK474 is a triazine derivative that acts as an inhibitor of class I phosphatidylinositol 3-kinase (PI3K) isoforms (IC50s = 17, 53, and 6 nM for p110β, -γ, and -δ, respectively). It is selective for PI3K, as it has negligible activity against 139 other kinases when tested at 30 μM. ZSTK474 is orally bioavailable and shows strong antitumor activity against human cancer xenografts in mice. The efficacy of ZSTK474 against certain cancer cells and tumors can be enhanced by combination therapy.
Verwenden
ZSTK474 is an ATP-competitive inhibitor of class I phosphatidylinositol 3 kinase (PI3K) isoforms. Potent PI3K inhibitor.
Definition
ChEBI: A triamino-1,3,5-triazine that is 1,3,5-triazine in which two of the hydrogens have been replaced by morpholin-4-yl groups while the third hydrogen has been replaced by a 2-(difluoromethyl)benzimidazol-1-yl group. It is an inhibitor of phosphatidylinositol 3-kinase.
target
PI3Kδ
Einzelnachweise
1) Kong and Yamori et al. (2007), ZSTK474 is an ATP-competitive inhibitor of class I phosphatidylinositol 3 kinase isoforms; Cancer Sci., 98 1638 2) Yaguchi et al. (2006), Antitumor activity of ZST474, a new phosphatidylinositol 3-kinase inhibitor; J. Natl. Cancer Inst., 98 545 3) Xue et al. (2014), ZSTK474, a novel PI3K inhibitor, modulates human CD14+ monocyte-derived dendritic cell functions and suppresses experimental autoimmune encephalomyelitis; J. Mol. Med. (Berl.), 92 1057 4) Haruta et al. (2012), Inhibitory effects of ZST474, a phosphatidylinositol 3-kinase inhibitor, on adjuvant-induced arthritis in rats; Inflamm. Res., 61 551

ZSTK474 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

475110-96-4, ZSTK474 Verwandte Suche:

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