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PDK1/Akt/Flt Dual Pathway Inhibitor，5MG，521275-5MGCN，Sigma

销售价： ¥ 3527.23 / 件

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订货号： 0BV4149

品牌型号： Sigma 521275-5MGCN

货期：询货期

最小订货量： 1件

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商品介绍
规格参数
包装参数

产品介绍 Product Description

General description

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 in in vitro kinase assays in a dose-dependent manner and block cellular phosphorylation of Akt at both Ser⁴⁷³ and 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 µM 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)

Biochem/physiol Actions

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 µM for AML with wild-type Flt3, single mutant ITD/D835, and double mutant Flt3-ITD-TDK, respectively

Packaging

Packaged under inert gas

Other Notes

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.

Legal Information

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

Disclaimer

Toxicity: Irritant (B)

技术参数 Specifications

Quality Segment	100
assay	≥98% (sum of two isomers, HPLC)
form	solid
manufacturer/tradename	Calbiochem^®
storage condition	OK to freeze,protect from light
color	yellow
solubility	DMSO: 10 mg/mL
shipped in	ambient
storage temp.	2-8°C
SMILES string	[n]21nnnc2nc3c(n1)c4c(cccc4)C3=O
InChI	1S/C10H4N6O/c17-9-6-4-2-1-3-5(6)7-8(9)11-10-12-14-15-16(10)13-7/h1-4H
InChI key	SSNMLKNJEUSPDY-UHFFFAOYSA-N

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