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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Phospholipase-ABD778
ABD778

Chemical Structure : ABD778

CAS No.:

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ABD778 (ABD-778)

货号: PC-24356Not For Human Use, Lab Use Only.

ABD778 is a potent and selective, in vivo-active ABHD17 inhibitor with IC50 of 76 nM and 84 nM for both human and mouse ABHD17 enzymes, respectively, is the isopropyl ester analog of ABD957.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

ABD778 is a potent and selective, in vivo-active ABHD17 inhibitor with IC50 of 76 nM and 84 nM for both human and mouse ABHD17 enzymes, respectively, is the isopropyl ester analog of ABD957.
ABD778 demonstrates high specificity for ABHD17 enzymes across the detectable serine hydrolases in both mouse and human proteomes.
ABD778 potently inhibits all ABHD17 isoforms in OCI-AML3 cells while maintaining a similar selectivity profile as observed in cell lysates.
ABD778 selectively reduces the growth of NRAS-mutant leukemia cells and is synergistic with PD901 in vitro.
ABD778 significantly reduced both cytokine-independent and GM-CSF-stimulated colony growth of JMML cells with NRAS mutations but had no effect on KRAS-mutant cells.
ABD778 augmented the anti-leukemia activity of the pan-PI3 kinase inhibitor pictilisib, the K/N-RasG12C inhibitor sotorasib, and the FLT3 inhibitor gilteritinib in a patient-derived xenograft model of adaptive resistance to FLT3 inhibition.

物理化学性质&存储条件

分子量 669.77
分子式 C30H42F3N7O5S
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

isopropyl 2-(8-(2-(((S)-4-(3-(N,N-dimethylsulfamoyl)-1H-pyrazole-1-carbonyl)-3-methylpiperazin-1-yl)methyl)-5-(trifluoromethyl)phenyl)-3,8-diazabicyclo[3.2.1]octan-3-yl)acetate

参考文献

1. Decker M, et al. bioRxiv, 2025 Mar 21:2025.03.20.644389.

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