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首页-抗体药物偶连体和PROTACs-PROTAC-PD-305
PD-305

Chemical Structure : PD-305

CAS No.: 3131845-75-2

PD-305 (PD305)

货号: PC-28644Not For Human Use, Lab Use Only.

PD-305 is a potent, selective PTPN2 (TCPTP) PROTAC degrader with DC50 of 0.25 nM in Jurkat cell line, possessing 20-fold PTPN2/PTPN1 subtype selectivity (PTPN1, DC50=5.11 nM).

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

PD-305 is a potent, selective PTPN2 (TCPTP) PROTAC degrader with DC50 of 0.25 nM in Jurkat cell line, possessing 20-fold PTPN2/PTPN1 subtype selectivity (PTPN1, DC50=5.11 nM).
PD-305 induces subtype-selective PTPN2 degradation in the B16F10 mouse melanoma cell line, has little or no effect on PTPN1 levels in this cell line.
PD-305 has no observable effect on IKZF1/3 levels.
PD-305 potently inhibits HT-29 proliferation with IC50 of 11.95 nM, 80-fold more potent than AC484.
PD-305 significantly upregulates the phosphorylation level of LCK, amplify IFN-γ-induced HT-29 human colorectal cancer cell growth inhibition and promotes T-cell activation.
PD-305 possesses excellent in vivo PTPN2 degradation potency and effectively suppressed tumor growth in mice.

物理化学性质&存储条件

分子量 796.87
分子式 C41H41FN6O8S
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

3-(6-(1-(3-(3-((3-(1,1-Dioxido-4-oxo-1,2,5-thiadiazolidin-2-yl)-2-fluoro-4-hydroxy-6-methylphenyl)-ethynyl)-pyrrolidine-1-Carbonyl)-cyclobutyl)-piperidin-4-yl)-2-oxobenzo-[cd]-indol-1-(2H)-yl)-piperidine-2,6-dione

参考文献

1. Linghao Hu, et al. J Med Chem. 2026 May 28;69(10):11998-12019.

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