DC Chemicals · Product datasheet

Afuresertib HCl — Datasheet

CAT. NO. DC7994

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ParameterValue
Chemical NameAfuresertib hydrochloride
CAS No.1047645-82-8
SynonymsGSK 2110183 hydrochloride;Afuresertib hydrochloride;GSK2110183B;N-[(2S)-1-amino-3-(3-fluorophenyl)propan-2-yl]-5-chloro-4-(4-chloro-2-methylpyrazol-3-yl)thiophene-2-carboxamide,hydrochloride;N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecarboxamide hydrochloride;Afuresertib HCl;GSK-2110183 hydrochloride;UNII-0FC27E442O;GSK 2110183B;GSK-2110183B;GSK2110183 hydrochloride;Afuresertib (hydrochloride);Afuresertib HCl (GSK2110183);Afuresertib HCl salt, GSK-2110183 HCl salt, GSK-2110183B HCl salt;Afuresertib hydrochloride [USAN];0FC27E442O;Afuresertib hydrochloride (USAN);AK171367;YFQJOPFTGMHYNV-YDALLXLXSA-N;GSK2110183B; Afuresertib HCl;N-((S)-1-Amino-3-(3-fluorophenyl)propan-2-yl)-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)thiophene-2-carboxamide hydrochloride;BCP19741
FormulaC18H18Cl3FN4OS
M.Wt463.7841
SMILESClC1=C(C2=C(C([H])=NN2C([H])([H])[H])Cl)C([H])=C(C(N([H])[C@]([H])(C([H])([H])N([H])[H])C([H])([H])C2C([H])=C([H])C([H])=C(C=2[H])F)=O)S1.Cl[H]
Purity>98%
Storage2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Biological Activity

Afuresertib hydrochloride is a potent and ATP-competitive specific Akt inhibitor.

In Vitro

Afuresertib exhibits favorable tumor-suppressive effects on malignant pleural mesothelioma (MPM) cells. Afuresertib significantly increases caspase-3 and caspase-7 activities and apoptotic cell number among ACC-MESO-4 and MSTO-211H cells. Afuresertib strongly arrests the cell cycle in the G1 phase. Western blotting analysis shows that Afuresertib increases the expression of p21WAF1/CIP1 and decreases the phosphorylation of Akt substrates, including GSK-3β and FOXO family proteins. Afuresertib-induced p21 expression promotes G1 phase arrest by inducing FOXO activity. Afuresertib significantly enhances cisplatin-induced cytotoxicity. Afuresertib modulates the expression E2F1 and MYC, which are associated with fibroblast core serum response[1].

In Vivo

No in vivo data are provided in the current product source. Contact us for further information.

References & source

DC Chemicals original product information

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.

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