AES-135

SKU: orb1218347

Description

AES-135 is a potent HDAC inhibitor, inhibits HDAC3, HDAC6, HDAC11 (IC50s: 654, 190, and 636 nM) with anti-tumor activity.

Key Properties

• CAS Number: 2361659-61-0
• MW: 693.66
• Purity: >98% (HPLC)
• Formula: C₃₃H₂₉F₆N₃O₅S
• SMILES: CC(C)(C)C1=CC=C(C=C1)CN(C2=CC=C(C=C2)C(=O)NO)C(=O)CN(CC3=C(C(=C(C(=C3F)F)F)F)F)S(=O)(=O)C4=CC=C(C=C4)F
• Target: HDAC
• Solubility: DMSO:100 mg/mL (144.16 mM; Need ultrasonic)

Bioactivity

• 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 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. 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.
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• 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. 体:
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

HDAC