KP372-1 |
| Katalog-Nr.GC15553 |
KP372-1, ein Akt-Inhibitor, blockiert die SignalÜbertragung Über den PI3K-Signalweg und hemmt die Zellproliferation, wÄhrend es die Apoptose von Krebszellen induziert.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1374996-60-7
Sample solution is provided at 25 µL, 10mM.
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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).
| Cas No. | 1374996-60-7 | SDF | |
| Chemical Name | 6H-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) | ||
| Canonical SMILES | O=C(C1=C2C=CC=C1)C(C2=N3)=NN4C3=NN=N4.O=C5C6=NC7=NN=NN7N=C6C8=C5C=CC=C8 | ||
| Formula | C10H4N6O • C10H4N6O | M.Wt | 448.36 |
| Löslichkeit | ≤20mg/ml in DMSO;20mg/ml in dimethyl formamide | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.2304 mL | 11.1518 mL | 22.3035 mL |
| 5 mM | 446.1 μL | 2.2304 mL | 4.4607 mL |
| 10 mM | 223 μL | 1.1152 mL | 2.2304 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 8 reference(s) in Google Scholar.)
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