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首页-抗体药物偶连体和PROTACs-PROTAC-ABS-752 hydrochloride
ABS-752 hydrochloride

Chemical Structure : ABS-752 hydrochloride

CAS No.: 2922884-90-8

ABS-752 hydrochloride

货号: PC-25335Not For Human Use, Lab Use Only.

ABS-752 hydrochloride is a prodrug of ABT-002 that could be activated by the monoamine oxidase VAP-1, ABS-752 is a molecular glue degrader of GSPT1 and NEK7 with DC50 of 1 nM and 9 nM in Hep3B cells (24 h, Dmax>95%).

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

ABS-752 hydrochloride is a prodrug of ABT-002 that could be activated by the monoamine oxidase VAP-1, ABS-752 is a molecular glue degrader of GSPT1 and NEK7 with DC50 of 1 nM and 9 nM in Hep3B cells (24 h, Dmax>95%).
ABS-752 does not form ternary complexes with CRBN and the neosubstrates. VAP-1, which is overexpressed in cirrhotic liver, is identified as the primary monoamine oxidase responsible for the conversion of ABS-752.
ABS-752 is potent against Hep3B and profoundly impacts viability in 575, HLE, JHH-7, HuH-7, SNU-423, SNU-878, and KKU-M213 cell lines.
ABS-752 degrades SALL4, NEK7, CK1α, and GSPT1, but not IKZF1 (unlike Pomalidomide in H929 cells).
EK7 and CK1α shows much weaker degradation after 6 h compared to GSPT1, with DC50 values of approximately 100 nM and >1000 nM, respectively.
ABT-002 as the active metabolite of ABS-752.
ABS-752 (100 mg/kg ABS-752 BID, PO) significant inhibited tumor growth in HCC PDX models.

物理化学性质&存储条件

分子量 327.74
分子式 C14H15ClFN3O3
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

2,6-Piperidinedione, 3-[5-(aminomethyl)-6-fluoro-1,3-dihydro-1-oxo-2H-isoindol-2-yl]-, hydrochloride (1:1)

参考文献

1. Glaza P, et al. Commun Chem. 2025 Aug 14;8(1):247.

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