FPA 124Akt/PKB inhibitor CAS# 902779-59-3 |
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Quality Control & MSDS
3D structure
Package In Stock
Number of papers citing our products
| Cas No. | 902779-59-3 | SDF | Download SDF |
| PubChem ID | 16034833 | Appearance | Powder |
| Formula | C11H9Cl2CuN3O2S | M.Wt | 381.73 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 10 mM in DMSO and to 10 mM in ethanol | ||
| Chemical Name | dichlorocopper;[(E)-(4-oxochromen-3-yl)methylideneamino]thiourea | ||
| SMILES | C1=CC=C2C(=C1)C(=O)C(=CO2)C=NNC(=S)N.Cl[Cu]Cl | ||
| Standard InChIKey | HZRXQEVFXXQYFS-VBPDOGLUSA-L | ||
| Standard InChI | InChI=1S/C11H9N3O2S.2ClH.Cu/c12-11(17)14-13-5-7-6-16-9-4-2-1-3-8(9)10(7)15;;;/h1-6H,(H3,12,14,17);2*1H;/q;;;+2/p-2/b13-5+;;; | ||
| General tips | For 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. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Akt/PKB inhibitor (IC50 = 100 nM) that interacts with the PH and kinase domains. Inhibits cell proliferation in various cancer cell lines in vitro and decreases NF-κB activity and tumor load in vivo. |
FPA 124 Dilution Calculator
FPA 124 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.6197 mL | 13.0983 mL | 26.1965 mL | 52.3931 mL | 65.4913 mL |
| 5 mM | 0.5239 mL | 2.6197 mL | 5.2393 mL | 10.4786 mL | 13.0983 mL |
| 10 mM | 0.262 mL | 1.3098 mL | 2.6197 mL | 5.2393 mL | 6.5491 mL |
| 50 mM | 0.0524 mL | 0.262 mL | 0.5239 mL | 1.0479 mL | 1.3098 mL |
| 100 mM | 0.0262 mL | 0.131 mL | 0.262 mL | 0.5239 mL | 0.6549 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Synthesis, molecular characterization, and biological activity of novel synthetic derivatives of chromen-4-one in human cancer cells.[Pubmed:16789737]
J Med Chem. 2006 Jun 29;49(13):3800-8.
The synthesis and characterization of Schiff base derivatives of 3-formylchromone 3-6 (FPA-120 to FPA-123), the minimal biologically active structural motif of soy isoflavone, genistein, and their copper(II) complexes 7-10 (FPA-124 to FPA-127) are reported here. These copper complexes possess distorted square-planar geometries capable of stabilizing Cu2+/Cu+ redox forms. The molecular modeling study revealed that the key interaction of the metal complexes was with amino acids in the pleckstrin homology (PH) and the kinase domain of the PKB (Akt) protein. Copper complex 7 significantly forms stronger charge interactions in the kinase domain than genistein, leading to better stabilization in the active pocket. In vitro evaluation of copper complexes against hormone-independent and metastatic breast (BT20), prostate (PC-3), and K-ras mutant (COLO 357) and K-ras wild-type (BxPC-3) pancreatic cancer cells revealed that 7 was the most potent compound which exhibited PKB (Akt protein) inhibitory activities and caused NF-kappaB inactivation in a well-established orthotopic pancreatic tumor model using COLO 357 cells. An inverse relationship was observed between IC50 values of the anti-proliferative activities and the Cu2+/Cu+ redox couple for these compounds, which may provide a rapid screen for evaluating the efficacy of active metallodrugs affecting redox-sensitive transcription factors such as NF-kappaB and its upstream target, the PKB (Akt) pathway, in multiple cancers.
