Ceranib-2 is a potent non-lipid ceramidase inhibitor that can suppress cellular ceramidase activity in SKOV3 cells with IC50 of 28 μM. Ceranib-2 can induce the accumulation of a variety of ceramide substances, reduce the levels of sphingosine and sphingosine 1-phosphate (S1P), and cause apoptosis. anti-cancer effect.

Physicochemical Properties

Molecular Formula	C₂₅H₁₉NO₃
Molecular Weight	381.42
Exact Mass	381.136
CAS #	1402830-75-4
Appearance	White to yellow solid powder
Density	1.2±0.1 g/cm3
Boiling Point	629.2±55.0 °C at 760 mmHg
Flash Point	334.4±31.5 °C
Vapour Pressure	0.0±1.8 mmHg at 25°C
Index of Refraction	1.657
LogP	4.9
Synonyms	Ceranib2; Ceranib 2
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	Ceranib-2 treatment (10 nM-10 µM; 72 hours; SKOV3 cells) reduces the growth and/or survival of cells, with an IC50 value of 0.73 µM [1]. After 48 hours of treatment with ceretib-2 (0.75-1.5 µM; SKOV3 cells), cells accumulate in the sub-G1 (apoptotic), G2, and S (0.75 µM only) phases of the cell cycle, resulting in a drop in total cell quantity. G1 phase cells [1]. Ceranib-2 inhibits ceramidase activity in a dose-dependent manner, causing a 50% drop at 28 μM. It also induces the buildup of various ceramide species and lowers levels of sphingosine and S1P [1].
ln Vivo	Treatment with Ceranib-2 (20–50 mg/kg; i.p.; once daily, five days a week; for three weeks; female Balb/c mice) in syngeneic tumor models slows the growth of tumors without hematologic suppression or overt toxicity [1]. After administering 50 mg/kg of Ceranib-2 intraperitoneally, the levels gradually increased and at the 2-hour mark, the peak plasma concentration was approximately 40 μM. Ceranib-2's half-life of less than two hours suggests that it is removed [1].
Cell Assay	Cell Proliferation Assay[1] Cell Types: SKOV3 Cell Tested Concentrations: 10 nM-10 µM Incubation Duration: 72 hrs (hours) Experimental Results: Ceranib-2 inhibits cell proliferation and/or survival with an IC50 value of 0.73 µM. Cell cycle analysis[1] Cell Types: SKOV3 Cell Tested Concentrations: 0.75 μM or 1.5 μM Incubation Duration: 48 hrs (hours) Experimental Results: Induction of cell cycle arrest and cell death.
Animal Protocol	Animal/Disease Models: Female balb/c (Bagg ALBino) mouse were injected with JC mouse breast cancer cells [1] Doses: 20 mg/kg or 50 mg/kg Route of Administration: intraperitoneal (ip) injection; one time/day, 5 days a week; for 3 weeks. Experimental Results: Same Delayed tumor growth in genetic tumor models.
References	[1]. Discovery and evaluation of inhibitors of human ceramidase. Mol Cancer Ther. 2011 Nov;10(11):2052-61. [2]. Induction of apoptosis in prostate cancer cells by the novel ceramidase inhibitor ceranib-2. In Vitro Cell Dev Biol Anim. 2015 Nov;51(10):1056-63.

Solubility Data

Solubility (In Vitro)

DMSO : ~50 mg/mL (~131.09 mM)

Solubility (In Vivo)

Solubility in Formulation 1: 2.5 mg/mL (6.55 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% 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 25.0 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: 2.5 mg/mL (6.55 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 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	2.6218 mL	13.1089 mL	26.2178 mL
	5 mM	0.5244 mL	2.6218 mL	5.2436 mL
	10 mM	0.2622 mL	1.3109 mL	2.6218 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.