AES-350

SKU: orb1217598

Description

AES-350 is a potent and orally active HDAC6 inhibitor(IC50 and a Ki of 0.0244 μM and 0.035 μM, respectively). It is also against HDAC-3, -8, and -11 in an enzymatic activity assay with IC50 values of 0.187 μM, 0.245 μM, and >1μM, respectively. AES-350 triggers apoptosis in AML cells through HDAC inhibition and can be used for acute myeloid leukemia (AML) research.

Images & Validation

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Key Properties

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CAS Number	847249-57-4
MW	312.36
Purity	>98% (HPLC)
Formula	C₁₈H₂₀N₂O₃
SMILES	CC(C)(C)C1=CC=C(C(NC2=CC=C(C(NO)=O)C=C2)=O)C=C1
Target	HDAC
Solubility	DMSO:100 mg/mL (320.14 mM; Need ultrasonic)

Bioactivity

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In Vivo

AES-350 (oral gavage; 20 mg/kg; single dose) exhibits a relative good pharmacokinetic (PK) properties in CD-1 mice. The single dose oral bioavailability (F%) of 51 is 19.8%. In comparison, the reported F% for SAHA in mice is significantly lower (8%).

In Vitro

In contrast, AES-350 has submicromolar activity (IC50 = 0.58±0.13 μM) against MV4-11 cells than to that of vorinostat (IC50 = 0.31±0.061 μM). AES-350 is more ligand efficient and exemplifies a large therapeutic index (IC50>30 μM in noncancerous MRC-9 cells). AES-350 is also shown to be effective in AML-3 (acute myeloid leukemia) cells (IC50 = 0.73 ± 0.12 μM). AES-350 (0.25-4 μM; 18 hours) induces MV4-11 cells apoptosis in a dose-dependent manner. The late apoptosis ratios are 8.74%, 11.7%, 16.08%, 30.97%, and 38.48%, respectively at 0.25 μM-4 μM. An ELISA is performed using HeLa cervical cancer cell lysates, and HeLa cells highly express HDAC6 and are sensitive to AES-350. Correspondingly, ELISA assays depicted a dose-dependent increase in HDAC6 inhibition (IC50 = 0.58±0.13 μM), Western blot analysis shows that AES-350 (0.1-10 μM) induces a dose-dependent increase in acetylated α-tubulin (Ac-α-tubulin), a substrate of HDAC. Apoptosis Analysis Cell line: MV4-11 cells. Concentration: 0.25 μM; 0.5 μM; 1.00 μM; 2.00 μM; 4.00 μM Incubation time: 18 hours. Result: Revealed a clear dosedependent increase in the percentage of cells entering late-stage apoptosis, similar to SAHA.

Storage & Handling

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

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AES-350 (orb1217598)

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Clonality:	Monoclonal
Conjugation:	Unconjugated

Purity:	99.20% (May vary between batches)
CAS Number:	847249-57-4
MW:	312.36
Formula:	C₁₈H₂₀N₂O₃

AES-350

Description

Images & Validation

Key Properties

Bioactivity

Storage & Handling

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AES-350 (orb1217598)

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