产品说明
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 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)
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 µM 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
基本信息
经验(实验)分子式 | C10H4N6O |
分子量 | 224.18 |
产品性质
质量水平 | 100 |
测定 | ≥98% (sum of two isomers, HPLC) |
形式 | solid |
manufacturer/tradename | Calbiochem® |
储存条件 | OK to freeze protect from light |
颜色 | yellow |
溶解性 | DMSO: 10 mg/mL |
运输 | ambient |
储存温度 | 2-8℃ |
安全信息
储存分类代码 | 10-13 - German Storage Class 10 to 13 |
Sigma-Aldrich