SE-7552

CAS: 2243575-79-1 F: C15H12F3N5O W: 335.28

SE-7552, a 2-(difluoromethyl)-1,3,4-oxadiazole (DFMO) derivative, is an orally active, highly selective, non-hydroxamate

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Bioactivity	SE-7552, a 2-(difluoromethyl)-1,3,4-oxadiazole (DFMO) derivative, is an orally active, highly selective, non-hydroxamate HDAC6 inhibitor with an IC50 of 33 nM. SE-7552 is greater than 850-fold selectivity versus all other known HDAC isozymes. SE-7552 is capable of blocking multiple myeloma growth in vivo. SE-7552 acts as an anti-obesity agent in diet-induced obese mice[1][2].
In Vivo	SE-7552 (30 mg/kg；单次口服灌胃) 可在小鼠体内增加乙酰化 α-微管蛋白水平超过 24 小时。SE-7552 对 H3 的乙酰化 (抑制 I 类 HDAC 的生物标志物) 没有影响[1]。SE-7552 (10 mg/kg；口服灌胃；每日) 与泊马度胺 (HY-10984；1 mg/kg；每日腹腔注射)联合使用，与单独泊马度胺组相比，在含有人 H929 MM 细胞的小鼠中可显着延迟肿瘤生长，并增强存活率[1]。SE-7552 表现出优异的 PK，小鼠单次口服剂量 5 mg/kg 后的最大暴露量为 597 ng/ml，半衰期为 7.2 小时[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only.
CAS	2243575-79-1
Formula	C15H12F3N5O
Molar Mass	335.28
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Jason A Holt, et al. 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]. Beate König, et al. 2-(Difluoromethyl)-1,3,4-oxadiazoles: The Future of Selective Histone Deacetylase 6 Modulation? ACS Pharmacol. Transl. Sci. 2024, February 20.