1. Cell Cycle/DNA Damage
    Epigenetics
  2. HDAC
  3. AES-135

AES-135 

Cat. No.: HY-114483 Purity: 98.31%
Handling Instructions

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.

For research use only. We do not sell to patients.

AES-135 Chemical Structure

AES-135 Chemical Structure

CAS No. : 2361659-61-0

Size Price Stock Quantity
5 mg USD 400 In-stock
Estimated Time of Arrival: December 31
10 mg USD 680 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1350 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2200 In-stock
Estimated Time of Arrival: December 31
100 mg USD 3400 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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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].

IC50 & Target[1]

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].

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[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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

693.66

Formula

C₃₃H₂₉F₆N₃O₅S

CAS No.

2361659-61-0

SMILES

CC(C)(C)C1=CC=C(CN(C(CN(CC2=C(F)C(F)=C(F)C(F)=C2F)S(=O)(C3=CC=C(F)C=C3)=O)=O)C4=CC=C(C(NO)=O)C=C4)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (144.16 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.4416 mL 7.2081 mL 14.4163 mL
5 mM 0.2883 mL 1.4416 mL 2.8833 mL
10 mM 0.1442 mL 0.7208 mL 1.4416 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (3.60 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

AES-135AES135AES 135HDACHistone deacetylasesHDAC3HDAC6HDAC11anti-tumorpancreaticInhibitorinhibitorinhibit

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Product Name:
AES-135
Cat. No.:
HY-114483
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