ALEXIS Biochemicals: ZSTK474

ALX-270-454

Revised 26-Mar-07

ZSTK474
SYNONYMS	2-(2-Difluoromethylbenzimidazol-1-yl)-4,6-dimorpholino-1,3,5-triazine
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	Phosphoinositide 3-kinase [PI(3)K] / Related Products

Ordering Information

not sold in USA

Product Specification

FORMULA:	C₁₉H₂₁F₂N₇O₂
MW:	417.4
CAS NUMBER:	475110-96-4
PURITY:	≥98% (HPLC)
APPEARANCE:	White to off-white solid.
SOLUBILITY:	Soluble in DMSO.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
USE/STABILITY:	Stock solutions are stable for up to 6 months when stored at -20°C.
HANDLING:	Protect from light.
HAZARD:	IRRITANT.

Product Description

Cell permeable, reversible, potent and specific inhibitor of phosphoinositide 3-kinase (IC₅₀=17nM for PI(3)K p110β, IC₅₀=53nM for PI(3)K p110γ and IC₅₀=6nM for PI(3)K p110δ). Blocks cellular PI(3)K/Akt (PKB) signalling in vitro and inhibits Akt(PKB)-dependent tumor growth in mice in vivo without significant toxic effect. More effective than LY 294,002 (Prod. No. ALX-270-038) in vitro and as in vivo.

Product Specific Literature References

A novel phosphatidylinositol 3-kinase inhibitor, ZSTK474 exerted antitumor activity against human tumor xenografts by oral administration: S.Yaguchi et al.; Proc. Am. Assoc. Cancer Res. 46, 1691 (2005)
Antitumor activity of ZSTK474, a new phosphatidylinositol 3-kinase inhibitor: S. Yaguchi, et al.; J. Natl. Cancer Inst. 98, 545 (2006) Abstract