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.
别名:
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
质量水平
方案
≥98% (sum of two isomers, HPLC)
表单
solid
制造商/商品名称
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°C
SMILES字符串
[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
相关类别
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. CAS. No. 331253-86-2 and 329710-24-9.
CAS. Nos. 331253-86-2 and 329710-24-9 (two isomers)
生化/生理作用
Cell permeable: yes
Primary Target
Both PDK1 and Akt activities
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
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.
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
免责声明
Toxicity: Irritant (B)
储存分类代码
10-13 - German Storage Class 10 to 13
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