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ChemicalBook--->CAS DataBase List--->847249-57-4

847249-57-4

847249-57-4 Structure

847249-57-4 Structure
IdentificationBack Directory
[Name]

AES-350
[CAS]

847249-57-4
[Synonyms]

AES-350
Histone deacetylases,AES 350,MV4-11,AES-350,Apoptosis,acute myeloid leukemia,AML,Inhibitor,inhibit,AES350,HDAC
[Molecular Formula]

C18H20N2O3
[MDL Number]

MFCD34180323
[MOL File]

847249-57-4.mol
[Molecular Weight]

312.36
Chemical PropertiesBack Directory
[density ]

1.218±0.06 g/cm3(Predicted)
[storage temp. ]

4°C, protect from light
[solubility ]

DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS (pH 7.2) (1:3): 0.25 mg/ml,Ethanol: 1 mg/ml
[form ]

A crystalline solid
[pka]

8.93±0.10(Predicted)
[color ]

Off-white to light yellow
Hazard InformationBack Directory
[Uses]

AES-350 is a potent and orally active HDAC6 inhibitor with an IC50 and a Ki of 0.0244 μM and 0.035 μM, respectively. AES-350 is also against HDAC3, HDAC8 in an enzymatic activity assay with IC50 values of 0.187 μM and 0.245 μM, respectively. AES-350 triggers apoptosis in AML cells through HDAC inhibition and can be used for acute myeloid leukemia (AML) research[1].
[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%)[1].

[IC 50]

HDAC6: 24.4 nM (IC50); HDAC3: 187 nM (IC50); HDAC11: 245 nM (IC50)
[storage]

4°C, protect from light
[References]

[1] Andrew E Shouksmith, et al. Class I/IIb-Selective HDAC Inhibitor Exhibits Oral Bioavailability and Therapeutic Efficacy in Acute Myeloid Leukemia. DOI:10.1021/acsmedchemlett.9b00471
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