Aminoxyrone (AX)

Chemical Structure : Aminoxyrone

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货号: PC-63505Not For Human Use, Lab Use Only.

Aminoxyrone (AX) is a novel peptidometic C-terminal HSP90 inhibitor by targeting HSP90 dimerization via the C-terminal domain (CTD) with Kd of 27.4 uM.

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生物&药学活性

Aminoxyrone (AX) is a novel peptidometic C-terminal HSP90 inhibitor by targeting HSP90 dimerization via the C-terminal domain (CTD) with Kd of 27.4 uM.
Aminoxyrone destabilizes BCR-ABL1 without inducing HSR in vitro and in vivo, additionally reduces pAKT-S473, pS6 expression and expression of client proteins associated with HSP90 chaperone activity, involving t-AKT, t-STAT5a, t-CRKL, cMYC, and BCL2.
Aminoxyrone triggers the degradation of HSP90 client proteins without elevating the expression of HSPs (HSP70, HSP40 & HSP27).
Aminoxyrone significantly inhibits cell growth and induces apoptosis of human leukemic stem cells (LSCs) with average EC50 of 20.94 uM.
Aminoxyrone is effective in imatinib resistant CML and lacks heat shock response.

物理化学性质&存储条件

分子量	994.153
分子式	C50H71N7O14
外观性状	Solid
CAS No.
储存条件	固体粉末 -20 °C 12 个月; 4°C 6 个月	配置液 -80 °C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	benzyl (((2R,6R,10R,14R,18R,22R)-6-benzyl-10,14-di((S)-sec-butyl)-22-carbamoyl-18-isobutyl-24-methyl-3,7,11,15,19-pentaoxo-1-phenyl-5,9,13,17,21-pentaoxa-4,8,12,16,20-pentaazapentacosan-2-yl)oxy)carbamate

参考文献

1. Bhatia S, et al. Blood. 2018 May 3. pii: blood-2017-10-810986.

Aminoxyrone (AX)

生物&药学活性

物理化学性质&存储条件

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Aminoxyrone (AX)

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