ZSTK474

ALX-270-454

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Inhibits all four PI3K isoforms.

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. BML-ST420) in vitro and as in vivo.

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Product Details

Alternative Name	2-(2-Difluoromethylbenzimidazol-1-yl)-4,6-dimorpholino-1,3,5-triazine
Appearance	White powder.
CAS	475110-96-4
Couple Target	PI3 kinase
Couple Type	Inhibitor
Formula	C₁₉H₂₁F₂N₇O₂
Identity	Determined by EM-MS and NMR.
MW	417.4
Purity	≥98% (HPLC)
Solubility	Soluble in DMSO (21mg/ml). Sparingly soluble in ethanol (<1mg/ml).

Handling & Storage

Use/Stability	As indicated on product label or CoA when stored as recommended. Stock solutions are stable for up to 6 months when stored at -20°C.
Handling	Protect from light.
Long Term Storage	-20°C
Shipping	Ambient Temperature

Regulatory Status	RUO – Research Use Only

Inhibition of mTOR-kinase destabilizes MYCN and is a potential therapy for MYCN-dependent tumors: Vaughan, L., Clarke, P. A., et al.; Oncotarget 7, 57525 (2016), Abstract
Alternative dosing of dual PI3K and MEK inhibition in cancer therapy: Jokinen, E., Laurila, N., et al.; BMC Cancer 12, 612 (2012), Abstract
Antitumor activity of ZSTK474, a new phosphatidylinositol 3-kinase inhibitor: S. Yaguchi, et al.; J. Natl. Cancer Inst. 98, 545 (2006), Abstract
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), Abstract

Related Products

LY 294002

BML-ST420

PI3 kinase inhibitor

50 citations

Alternative Name	2-(4-Morpholinyl)-8-phenyl-4H-1-benzopyran-4-one
CAS	154447-36-6
Couple Type	Inhibitor
Purity	≥98% (HPLC)

Last modified: May 29, 2024

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ZSTK474

ALX-270-454

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