ZSTK474 Inhibitor CAS No. 475110-96-4

Cat. No.	Name	Size	Price
KI3077	ZSTK474	10 mg	$112
	ZSTK474	20 mg	$180
	ZSTK474	50 mg	$432
	ZSTK474	200 mg	$1106
	ZSTK474	1 g	$4422

Chemical Characteristic

Product Name	ZSTK474
CAS No.	475110-96-4
Molecular Weight	417.418
Formula	C₁₉H₂₁F₂N₇O₂
Chemical Name	2-(2-Difluoromethylbenzimidazol-1-yl)-4,6-dimorpholino-1,3,5-triazine
Smiles	n1c(nc(nc1N1CCOCC1)N1CCOCC1)n1c(nc2c1cccc2)C(F)F
Chemical Structure

Biological activities

ZSTK474 is an ATP-competitive pan-class I PI3K inhibitor. ZSTK474 inhibits all the four PI3K isoforms (PI3Kα, β, δ, and γ) with IC50s of 16, 44, 5 and 49 nM, respectively.^[1] ZSTK474 also inhibits the growth of HU-VECs with an IC50 of 146 nM.^[2] ZSTK474 shows antitumour and antiangiogenic activity in vitro and in vivo. In vitro, ZSTK474 inhibits the production of IFNγ and IL-17 in concanavalin A-activated T cells. Meanwhile, ZSTK474 inhibits the proliferation and PGE(2) production by fibroblast-like synovial cells (FLS).^[3] In RXF-631L cancer cells, ZSTK474 inhibits the expression of HIF-1α and secretion of VEGF. In HUVEC, ZSTK474 inhibits the cell growth, blocks VEGF-induced cell migration and the tube formation. Furthermore, ZSTK474 inhibits phosphorylation of Akt at submicromolar concentrations.^[2] In vivo, in the RXF-631L xenograft model, ZSTK474 significantly inhibits tumour growth without observable toxicity.^[4] In a rat model of rheumatoid arthritis (RA), ZSTK474 demonstrates prophylactic efficacy through inhibition of T cell and FLS functions.^[3]

Protocols

In vitro, ZSTK474 is dissolved in DMSO.^[3]

References

[1]Kong DX, et al. ZSTK474, a novel phosphatidylinositol 3-kinase inhibitor identified using the JFCR39 drug discovery system. Acta Pharmacol Sin. 2010, 31 (9):1189-1197. [2]Kong D, et al. Antiangiogenic effect of ZSTK474, a novel phosphatidylinositol 3-kinase inhibitor. Eur J Cancer. 2009, 45 (5): 857-865. [3]Haruta K, et al. Inhibitory effects of ZSTK474, a phosphatidylinositol 3-kinase inhibitor, on adjuvant-induced arthritis in rats. Inflamm Res. 2012, 61 (6): 551-562. [4]Kong D, et al. ZSTK474 is an ATP-competitive inhibitor of class I phosphatidylinositol 3 kinase isoforms. Cancer Sci. 2007, 98 (10): 1638-1642.

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