AES-135

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 In Vitro AES-135 inhibits cancer cells growth with IC 50 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: C57Bl/6 mice injected with KPC2 cells Dosage: 50 mg/kg Administration: Intraperitoneal injection; 5 days a week; for 1 month Result: Significantly increased survival of mice. Form:Solid IC50& Target:HDAC6 190 nM (IC 50 ) HDAC11 636 nM (IC 50 ) HDAC3 654 nM (IC 50 ) HDAC8 1100 nM (IC 50 )

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