PDK1/Akt/Flt Dual Pathway Inhibitor-CAS 331253-86-2-Calbiochem

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一般描述

A cell-permeable compound that selectively induces apoptosis in AML (Acute Myelogenous Leukemia) with little effect on normal CD34⁺AML progenitor cells. Shown to directly inhibit both PDK1 and Akt activities inin vitrokinase assays in a dose-dependent manner and block cellular phosphorylation of Akt at both Ser⁴⁷³and Thr³⁰⁸. The dual inhibition nature against both PDK1/Akt and Flt3/PIM signaling pathways allows effective killing of AML cells (Average IC₅₀= 1.05, 1.91, and 0.43 ?M for AML with wild-type Flt3, single mutant ITD/D835, and double mutant Flt3-ITD-TDK, respectively) that are otherwise resistant to inhibitors that target only the PDK1/Akt pathway.
A cell-permeable compound that selectively induces apoptosis in AML (Acute Myelogenous Leukemia) with little effect on normal CD34⁺AML progenitor cells. Shown to directly inhibit both PDK1 and Akt activities inin vitrokinase assays in a dose-dependent manner and block cellular phosphorylation of Akt at both Ser⁴⁷³and Thr³⁰⁸. The dual inhibition nature against both PDK1/Akt and Flt3/PIM signaling pathways allows effective killing of AML cells (Average IC₅₀= 1.05, 1.91, and 0.43 ?M for AML with wild-type Flt3, single mutant ITD/D835, and double mutant Flt3-ITD-TDK, respectively) that are otherwise resistant to inhibitors that target only the PDK1/Akt pathway. CAS. No. 331253-86-2 and 329710-24-9.
CAS. Nos. 331253-86-2 and 329710-24-9 (two isomers)

包装

5 mg in Plastic ampoule
Packaged under inert gas

生化/生理作用

Cell permeable: yes
Primary Target
Both PDK1 and Akt activities
Product does not compete with ATP.
Reversible: no
Target IC₅₀: 1.05, 1.91, and 0.43 ?M for AML with wild-type Flt3, single mutant ITD/D835, and double mutant Flt3-ITD-TDK, respectively

警告

Toxicity: Irritant (B)

其他说明

Zeng, Z., et al. 2006.Cancer Res.66,3737.
Koul, D., et al. 2006.Mol. Cancer Ther.5,637.
Mandal. M., et al. 2006.Oral Oncol.42,430.
Mandal. M., et al. 2005.Br. J. Cancer92,1899.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

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