SE-7552 is a 2-(difluoromethyl)-1,3,4-oxadiazole (DFMO) derivative and is an orally active, highly selective, non-hydroxamic acid HDAC6 inhibitor with an IC50 of 33 nM. SE-7552 is 850-fold more selective than all other known HDAC isozymes. SE-7552 is able to block the growth of multiple myeloma in vivo. SE-7552 acts as an anti-obesity agent in diet-induced obese mice.

Physicochemical Properties

Molecular Formula	C15H12F3N5O
Molecular Weight	335.28
CAS #	2243575-79-1
PubChem CID	135320929
Appearance	Solid powder
Hydrogen Bond Donor Count	1
Hydrogen Bond Acceptor Count	9
Rotatable Bond Count	5
Heavy Atom Count	24
Complexity	389
Defined Atom Stereocenter Count	0
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	HDAC6 33 nM (IC50)
ln Vivo	SE-7552 (30 mg/kg; single oral gavage) increased acetylated α-tubulin levels in mice for more than 24 hours. SE-7552 had no effect on H3 acetylation, a biomarker for class I HDAC inhibition[1]. SE-7552 (10 mg/kg; oral gavage; daily) combined with pomalidomide (HY-10984; 1 mg/kg; intraperitoneal injection daily) significantly delayed tumor growth and enhanced survival in mice bearing human H929 MM cells compared to pomalidomide alone[1]. SE-7552 exhibited excellent PK, with a maximum exposure of 597 ng/ml and a half-life of 7.2 hours in mice after a single oral dose of 5 mg/kg[1].
References	[1]. SE-7552, a Highly Selective, Non-Hydroxamate Inhibitor of Histone Deacetylase-6 Blocks Multiple Myeloma Growth In Vivo. Blood (2018) 132 (Supplement 1): 3215. [2]. 2-(Difluoromethyl)-1,3,4-oxadiazoles: The Future of Selective Histone Deacetylase 6 Modulation? ACS Pharmacol. Transl. Sci. 2024, February 20.

Solubility Data

Solubility (In Vitro)

DMSO : 100 mg/mL (298.26 mM; with sonication)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (7.46 mM)(Saturation unknown) in 10% DMSO 40% PEG300 5% Tween-80 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, add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix well; then add 50 μL Tween-80 to the above system and mix well; then add 450 μL saline to make it 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 (7.46 mM)(Saturation unknown) in 10% DMSO 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution, add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD in saline and mix well. *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	2.9826 mL	14.9129 mL	29.8258 mL
	5 mM	0.5965 mL	2.9826 mL	5.9652 mL
	10 mM	0.2983 mL	1.4913 mL	2.9826 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.