您的位置:首页 > 产品中心 > 331253-86-2, PDK1/Akt/Flt Dual Pathway Inhibitor-CAS 331253-86-2-Calbiochem
PDK1/Akt/Flt Dual Pathway Inhibitor-CAS 331253-86-2-Calbiochem
产品编号: | 4084126 |
规格: | 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. |
CAS NO: | 331253-86-2 |
包装规格: | 5 MG |
产品类别: | 进口试剂 |
品牌: | Sigma-Aldrich |
优惠价: | 立即咨询 |
产品别名
331253-86-2
PDK1/Akt/Flt Dual Pathway Inhibitor-CAS 331253-86-2-Calbiochem
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
基本信息
Empirical Formula【经验(实验)分子式】 | C10H4N6O |
Molecular weight | 224.18 |
General description【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) |
Biochem/physiol Actions【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 |
Warning【警告】 | Toxicity: Irritant (B) |
Other Notes【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. |
Legal Information【法律信息】 | CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany |
产品性质
Quality Level【质量水平】 | 100 |
Assay【测定】 | ≥98% (sum of two isomers, HPLC) |
form【形式】 | solid |
manufacturer/tradename | Calbiochem® |
storage condition【储存条件】 | OK to freeze protect from light |
color【颜色】 | yellow |
solubility【溶解性】 | DMSO: 10 mg/mL |
shipped in【运输】 | ambient |
storage temp.【储存温度】 | 2-8℃ |
packaging【包装】 | 5 mg in Plastic ampoule Packaged under inert gas |
安全信息
Storage Class Code【储存分类代码】 | 10-13 - German Storage Class 10 to 13 |