Modify Search
Select all
Products
Pages
Posts
Modify Search
Select all
Products
Pages
Posts

ZSTK474 | PI 3-kinase inhibitor

CAS:
475110-96-4
Catalog Number:
10-2180
Activity:
PI 3-kinase inhibitor
Chemical Name:
2-(2-Difluoromethylbenzoimidazol-1-yl)-4,6-dimorpholino-1,3,5-triazine
Molecular Weight:
417.41
Molecular Formula:
C19H21F2N7O2
Solubility:
Soluble in DMSO (up to 20 mg/ml) or in Ethanol (up to 2.5 mg/ml with warming).
Physical Properties:
White or off-white solid
Purity:
99% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
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.
Shipping Code:
RT

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.

References/Citations:

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 | PI 3-kinase inhibitor is also available in the Cellular Metabolism Library.
CAS:
475110-96-4
Catalog Number:
10-2180
Activity:
PI 3-kinase inhibitor
Chemical Name:
2-(2-Difluoromethylbenzoimidazol-1-yl)-4,6-dimorpholino-1,3,5-triazine
Molecular Weight:
417.41
Molecular Formula:
C19H21F2N7O2
Solubility:
Soluble in DMSO (up to 20 mg/ml) or in Ethanol (up to 2.5 mg/ml with warming).
Physical Properties:
White or off-white solid
Purity:
99% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
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.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

Add to Quote

Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee