Chemical Name: 2-(2-Difluoromethylbenzoimidazol-1-yl)-4,6-dimorpholino-1,3,5-triazine
PI 3-kinase inhibitor
Molecular Weight:
417.41
Purity:
99% by HPLC NMR (Conforms)
Form:
White or off-white solid
CAS Number:
[475110-96-4]
Formula:
C19H21F2N7O2
Application Notes:
Novel Class I phosphatidylinositol 3-kinase (PI3K) inhibitor. ZSTK474 is an ATP-competitive inhibitor of all four Class I PI3K isoforms. However, it inhibits PI3Kdelta most potently, with a Ki of 1.8 nM, while inhibiting the alpha, beta and gamma 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. It 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.
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