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164B8

Chemical Structure : 164B8

CAS No.: 3101950-55-1

164B8

货号: PC-26206Not For Human Use, Lab Use Only.

164B8 is a highly potent, covalent Pin1 inhibitor / degrader with IC50 of 4.65 nM, reacts with the Pin1 active-site residue Cys113, effectively induces Pin1 degradation both in cell and in vivo.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

164B8 is a highly potent, covalent Pin1 inhibitor / degrader with IC50 of 4.65 nM, reacts with the Pin1 active-site residue Cys113, effectively induces Pin1 degradation both in cell and in vivo.
164B8 (5 uM) induces duration of Pin1 degradation approximately 50% after 48 h in BxPC3 and KPC cells.
164B8 inhibits cell viability of MIA PaCa-2 cells and KPC cell lines with EC50 of 8.4 uM and 5.3 uM respectively.
164B8 (30 mg/kg, 60 mg/kg) caused significant, dose-dependent reduction in tumor burden in murine model of metastatic pancreatic cancer.

物理化学性质&存储条件

分子量 625.55
分子式 C31H34Cl2N6O4
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

(S)-N-((S)-3-(1H-indol-3-yl)-1-(methylamino)-1-oxopropan-2-yl)-1-((S)-3-(6-chloro-1H-indol-3-yl)-2-(2-chloroacetamido)propanoyl)piperidine-2-carboxamide

参考文献

1. Giulia Alboreggia, et al. Mol Ther Oncol. 2025 Nov 1;33(4):201078.

2. Patent US20250296955 A1.

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