FPA-124, a cell-permeable (penetrable) copper complex, is a selective Akt inhibitor (antagonist) with IC50 of 0.1 μM and interacts with the protein homology (PH) domain and kinase domain of Akt. FPA-124 causes apoptosis.

Physicochemical Properties

Molecular Formula	C11H9CL2CUN3O2S
Molecular Weight	381.73
Exact Mass	379.909
CAS #	902779-59-3
PubChem CID	56972210
Appearance	Light green to green solid powder
LogP	3.427
Hydrogen Bond Donor Count	2
Hydrogen Bond Acceptor Count	4
Rotatable Bond Count	2
Heavy Atom Count	20
Complexity	395
Defined Atom Stereocenter Count	0
SMILES	C1=CC=C2C(=C1)C(=O)C(=CO2)/C=N\NC(=S)N.Cl[Cu]Cl
InChi Key	HZRXQEVFXXQYFS-KHDHKOIVSA-L
InChi Code	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-;;;
Chemical Name	dichlorocopper;[(Z)-(4-oxochromen-3-yl)methylideneamino]thiourea
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

ln Vitro	In BT20, PC-3, COLO 357, and BxPC-3 cancer cell lines, FPA-124 demonstrates dose-dependent growth inhibitory effects with IC50s of 7, 10, 34, and 55 μM, respectively[1].
ln Vivo	In a well-established orthotopic pancreatic tumor model employing COLO 357 cells, FPA-124 promotes NF-κB inactivation and demonstrates PKB (Akt protein) inhibitory activities[1].
References	[1]. Synthesis, molecular characterization, and biological activity of novel synthetic derivatives of chromen-4-one in human cancer cells. J Med Chem. 2006 Jun 29;49(13):3800-8. [2]. Pioglitazone enhances collateral blood flow in ischemic hindlimb of diabetic mice through an Akt-dependent VEGF-mediated mechanism, regardless of PPARgamma stimulation. Cardiovasc Diabetol. 2009 Sep 8;8:49.

Solubility Data

Solubility (In Vitro)

DMSO : 5 mg/mL (13.10 mM) H2O : < 0.1 mg/mL

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 0.67 mg/mL (1.76 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 6.7 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 0.67 mg/mL (1.76 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 6.7 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.6197 mL	13.0983 mL	26.1965 mL
	5 mM	0.5239 mL	2.6197 mL	5.2393 mL
	10 mM	0.2620 mL	1.3098 mL	2.6197 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.