AES-135

Modify Date: 2024-01-14 16:06:21

AES-135 structure	Common Name	AES-135
	CAS Number	2361659-61-0	Molecular Weight	693.66
	Density	N/A	Boiling Point	N/A
	Molecular Formula	C₃₃H₂₉F₆N₃O₅S	Melting Point	N/A
	MSDS	N/A	Flash Point	N/A

Use of AES-135

AES-135, a hydroxamic acid-based HDAC inhibitor, prolongs survival in an orthotopic mouse model of pancreatic cancer. AES-135 inhibits HDAC3, HDAC6, HDAC8, and HDAC11 with IC50s ranging from 190-1100 nM[1].

Name	Benzamide, 4-[[[4-(1,1-dimethylethyl)phenyl]methyl][2-[[(4-fluorophenyl)sulfonyl][(2,3,4,5,6-pentafluorophenyl)methyl]amino]acetyl]amino]-N-hydroxy-

Description	AES-135, a hydroxamic acid-based HDAC inhibitor, prolongs survival in an orthotopic mouse model of pancreatic cancer. AES-135 inhibits HDAC3, HDAC6, HDAC8, and HDAC11 with IC50s ranging from 190-1100 nM[1].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> Cell Cycle/DNA Damage >> HDAC Signaling Pathways >> Epigenetics >> HDAC
Target	HDAC6:190 nM (IC50) HDAC11:636 nM (IC50) HDAC3:654 nM (IC50) HDAC8:1100 nM (IC50)
In Vitro	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[1].
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[1]. 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 Cmax 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[1]. Animal Model: C57Bl/6 mice injected with KPC2 cells[1] Dosage: 50 mg/kg Administration: Intraperitoneal injection; 5 days a week; for 1 month Result: Significantly increased survival of mice.
References	[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.

Molecular Formula	C₃₃H₂₉F₆N₃O₅S
Molecular Weight	693.66

Hazard Codes	Xi