521275  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, Akt Inhibitor XXI, PDK1 Inhibitor I, KP372-1

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64293 Darmstadt
Phone: +49 6151 72-0
Fax: +49 6151 72 2000


18 เมษายน 2557

Product number Qty/Pk Quantity Price
521275-5MG  5 mg  loading
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. Nos. 331253-86-2 and 329710-24-9 (two isomers)
Product information
Form Yellow solid
Molar mass 224.2
Protect from Light Yes
Packaged under inert gas Yes
Purity ≥98% by HPLC (sum of two isomers)
Solubility DMSO
Chemical formula C10H4N6O
CAS number 331253-86-2
Store and ship information
Storage +2°C to +8°C
Ship Ambient Temperature Only
Safety information
S Phrase S: 26-36

In case of contact with eyes, rinse immediately with plenty of water and seek medical advice.
Wear suitable protective clothing.
R Phrase R: 36/37/38

Irritating to eyes, respiratory system and skin.
PDK1/Akt/Flt Dual Pathway Inhibitor, molecular structure

© Merck KGaA, Darmstadt, Germany, 2557


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