CC260 is a selective PI5P4Kα and PI5P4Kβ inhibitor (antagonist) with Ki of 40 nM and 30 nM, respectively. CC260 does not inhibit or weakly inhibits other protein kinases such as Plk1 and RSK2. CC260 may be utilized in cellular energy metabolism, diabetes and cancer research.

Physicochemical Properties

Molecular Formula	C24H29CL2N5O2
Molecular Weight	490.43
Exact Mass	489.169
CAS #	2411088-26-9
PubChem CID	146347307
Appearance	Off-white to gray solid powder
LogP	6.5
Hydrogen Bond Donor Count	2
Hydrogen Bond Acceptor Count	6
Rotatable Bond Count	5
Heavy Atom Count	33
Complexity	678
Defined Atom Stereocenter Count	1
SMILES	N1=C2C(N(C)C(=O)[C@@H](CC3CCCC3)N2C2CCCC2)=CN=C1NC1=CC(Cl)=C(O)C(Cl)=C1
InChi Key	AEZJZTFWCDAUDF-LJQANCHMSA-N
InChi Code	InChI=1S/C24H29Cl2N5O2/c1-30-20-13-27-24(28-15-11-17(25)21(32)18(26)12-15)29-22(20)31(16-8-4-5-9-16)19(23(30)33)10-14-6-2-3-7-14/h11-14,16,19,32H,2-10H2,1H3,(H,27,28,29)/t19-/m1/s1
Chemical Name	(7R)-8-cyclopentyl-7-(cyclopentylmethyl)-2-(3,5-dichloro-4-hydroxyanilino)-5-methyl-7H-pteridin-6-one
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

Targets	Ki: 40 nM (PI5P4Kα) and 30 nM (PI5P4Kβ)[1]
ln Vitro	CC260 (20 μM) reduces S6K phosphorylation (Thr-389) by mTORC1 but increases Insulin-induced Akt phosphorylation at both Thr-308 and Ser-473 in cultured C2C12 myotubes[1]. Acetyl-CoA carboxylase (ACC) phosphorylation is greatly increased by CC260 (2.5 μM, 5 μM, 10 μM, and 20 μM) in a dose-dependent manner[1]. Treatment with CC260 decreases the ability of BT474 cells to withstand serum starvation; however, this ability can be restored by expressing the refractory mutant PI5P4Kβ[1]. Treatment with CC260 increases the generation of glycolytic ATP in BT474 cells[1].
References	[1]. Pharmacological inhibition of PI5P4Kα/β disrupts cell energy metabolism and selectively kills p53-null tumor cells. Proc Natl Acad Sci U S A. 2021 May 25;118(21):e2002486118.

Solubility Data

Solubility (In Vitro)

DMSO: 160 mg/mL (326.24 mM)

Solubility (In Vivo)

Solubility in Formulation 1: 4 mg/mL (8.16 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 sonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 40.0 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. Solubility in Formulation 2: ≥ 4 mg/mL (8.16 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 40.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.0390 mL	10.1951 mL	20.3903 mL
	5 mM	0.4078 mL	2.0390 mL	4.0781 mL
	10 mM	0.2039 mL	1.0195 mL	2.0390 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.