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.

• Synonim(y): 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
• Wzór empiryczny (zapis Hilla): C₁₀H₄N₆O
• Numer CAS: 331253-86-2
• Masa cząsteczkowa: 224.18
• Kod UNSPSC: 12352200
• NACRES: NA.32

Właściwości

• Poziom jakości: 100
• Próba: ≥98% (sum of two isomers, HPLC)
• Postać: solid
• producent / nazwa handlowa: Calbiochem^®
• warunki przechowywania: OK to freeze; protect from light
• kolor: yellow
• rozpuszczalność: DMSO: 10 mg/mL
• Warunki transportu: ambient
• temp. przechowywania: 2-8°C
• 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
• Klucz InChI: SSNMLKNJEUSPDY-UHFFFAOYSA-N

Opis

Opis ogólny

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)

Działania biochem./fizjol.

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

Opakowanie

Packaged under inert gas

Ostrzeżenie

Toxicity: Irritant (B)

Inne uwagi

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.

Informacje prawne

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

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Informacja o środkach bezpieczeństwa

• Kod klasy składowania: 10-13 - German Storage Class 10 to 13