AES-135 是一种基于羟肟酸的泛 HDAC 抑制剂，可延长胰腺癌原位小鼠模型的存活时间。AES-135 抑制 HDAC3、HDAC6、HDAC8 和 HDAC11，IC₅₀ 范围为190-1100 nM。

AES-135, a hydroxamic acid-based pan-HDAC inhibitor, prolongs survival in an orthotopic mouse model of pancreatic cancer. AES-135 inhibits HDAC3, HDAC6, HDAC8, and HDAC11 with IC 50 s ranging from 190-1100 nM.

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HDAC6 190 nM (IC50) HDAC11 636 nM (IC

AES-135 inhibits cancer cells growth with IC50 values of 2.3 μM, 1.4 μM, 0.27 μM, 0.94 μM, 1.9 μM, 2.72 μM, 2.1 μM, 15.0 μM, 1.6 μM and 19.2 μM for BT143, BT189, D425, D458, MV4-11, MOLM-13, MDA-MB-231, K562, PC-3 and MRC-9 cells, respectively. has not independently confirmed the accuracy of these methods. They are for reference only.

AES-135 (50 mg/kg; intraperitoneal injection; 5 days a week; for 1 month) treatment significantly increases survival of C57Bl/6 mice implanted with KPC2 cells.
NSG mice are dosed with a single 20 mg/kg intraperitoneal (IP) injection, and blood is taken at 0.5 h, 1 h, 2 h, 4 h, 8 h, and 24 h. AES-135 achieved μM concentrations in the blood, reaching C max 7452 ng/mL (10.74 μM) within 30 min, which is sustained for 8 h. The blood concentration of AES-135 is dose dependent, achieving an average of 323 ng/mL (0.47 μM) with 10 mg/kg dosing and 1829 ng/mL (2.64 μM) with 40 mg/kg. AES-135 shows an impressive pharmacokinetic profile in mice with an in vivo half-life of 5.0 h. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Shouksmith AE, et al. Identification and Characterization of AES-135, a Hydroxamic Acid-Based HDAC Inhibitor That Prolongs Survival in an Orthotopic Mouse Model of Pancreatic Cancer. J Med Chem. 2019 Mar 14;62(5):2651-2665.

In Vitro: DMSO : 100 mg/mL (144.16 mM; Need ultrasonic)配制储备液