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 XIX; PDK1 Inhibitor I
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16 May 2012
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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
Irritant |
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| 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. |
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| R Phrase |
R: 36/37/38 Irritating to eyes, respiratory system and skin. |
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