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KP372-1

In stock
Catalog No.
C5053
specific Akt inhibitor
Grouped product items
SizePriceStock Qty
1mg
$71.00
In stock
5mg
$319.00
In stock
10mg
$566.00
In stock

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Email: [email protected]

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Background

IC50: 30-60 nM for thyroid cancer cells

KP372-1 is a specific Akt inhibitor.

The phosphatidylinositol 3' kinase (PI3K)/phosphatase, which is a key regulator of cell proliferation and survival, is mutated or activated in various cancers. Akt seems to be a key central node in this pathway and therefore is an promising target.

In vitro: A previous study found that KP372-1 could block signalling downstream of Akt in thyroid tumour cells, resulting in inhibition of cell proliferation and increased apoptosis [1]. Another study showed that KP372-1 directly inhibited the kinase activity of AKT, FLT3, and PDK1concentration-dependently. Western blot analyses indicated KP372-1 decreased the phosphorylation of AKT on both Ser(473) and Thr(308). Moreover, the treatment of AML cell lines with KP372-1 led to rapid generation of reactive oxygen species and stimulation of oxygen consumption. In addition, KP372-1 was able to induce pronounced apoptosis in AML cell lines and primary samples irrespective of their FLT3 status, but not in normal CD34(+) cells [2].

In vivo: Up to now, there is no animal in vivo data reported.

Clinical trial: So far, no clinical study has been conducted.

References:
[1] Mandal, M. ,Kim, S.,Younes, M.N., et al. The Akt inhibitor KP372-1 suppresses Akt activity and cell proliferation and induces apoptosis in thyroid cancer cells. British Journal of Cancer 92(10), 1899-1905 (2005).
[2] Zeng, Z. ,Samudio, I.J.,Zhang, W., et al. Simultaneous inhibition of PDK1/AKT and Fms-like tyrosine kinase 3 signaling by a small-molecule KP372-1 induces mitochondrial dysfunction and apoptosis in acute myelogenous leukemia. Cancer Research 66(7), 3737-3746 (2006).

Chemical Properties

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt224.2
Cas No.1374996-60-7
FormulaC10H4N6O • C10H4N6O
Solubility≤20mg/ml in DMSO;20mg/ml in dimethyl formamide
Chemical Name6H-​indeno[1,​2-​ε]​tetrazolo[1,​5-​b]​[1,​2,​4]​triazin-​6-​one, compd. with 10H-​indeno[2,​1-ε]​tetrazolo[1,​5-​b]​[1,​2,​4]​triazin-​10-​one (1:1)
SDFDownload SDF
Canonical SMILESO=C(C1=C2C=CC=C1)C(C2=N3)=NN4C3=NN=N4.O=C5C6=NC7=NN=NN7N=C6C8=C5C=CC=C8
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Quality Control

Quality Control & MSDS

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Chemical structure

KP372-1