521275

PDK1/Akt/Flt Dual Pathway Inhibitor

The PDK1/Akt/Flt Dual Pathway Inhibitor, also referenced under CAS 331253-86-2, controls the biological activity of PDK1/Akt/Flt. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• 別名: PDK1/Akt/Flt Dual Pathway Inhibitor, 6H-Indeno[1,2-e]tetrazolo[1,5-b][1,2,4]triazin-6-one & 10H-Indeno[2,1-e]tetrazolo[1,5-b][1,2,4]triazin-10-one, KP372-1, Akt Inhibitor XXI, PDK1 Inhibitor I
• 実験式（ヒル表記法）: C₁₀H₄N₆O
• CAS番号: 331253-86-2
• 分子量: 224.18
• UNSPSCコード: 12352200

特性

• 品質水準: 100
• アッセイ: ≥98% (sum of two isomers, HPLC)
• 形状: solid
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: yellow
• 溶解性: DMSO: 10 mg/mL
• 輸送温度: ambient
• 保管温度: 2-8°C
• 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

詳細

詳細

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.

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)

生物化学的／生理学的作用

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

包装

Packaged under inert gas

警告

Toxicity: Irritant (B)

その他情報

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.

法的情報

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

安全性情報

• 保管分類コード: 10-13 - German Storage Class 10 to 13