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PHGDH inhibitor D5-2

Chemical Structure : PHGDH inhibitor D5-2

CAS No.:

PHGDH inhibitor D5-2

货号: PC-27040Not For Human Use, Lab Use Only.

PHGDH inhibitor D5-2 is a selective, covalent inhibitor of PHGDH (MST Kd=3.4 uM) engaging the interfacial Cys281, potently disrupts PHGDH dimerization and inhibits its enzymatic activity.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

PHGDH inhibitor D5-2 is a selective, covalent inhibitor of PHGDH (MST Kd=3.4 uM) engaging the interfacial Cys281, potently disrupts PHGDH dimerization and inhibits its enzymatic activity.
D5-2 restores sensitivity to EGFR tyrosine kinase inhibitors in resistant lung adenocarcinoma cells in vitro, and exhibits antitumor efficacy in mouse xenograft models.

物理化学性质&存储条件

分子量 596.74
分子式 C32H40N10O2
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)-2-((4-(2-(but-2-ynoyl)-2,8-diazaspiro[4.5]decan-8-yl)-6-(methylamino)-1,3,5-triazin-2-yl)amino)-3-(4-(6-(dimethylamino)pyridin-3-yl)phenyl)propanamide

参考文献

1. Feng L, et al. J Med Chem. 2026 Jun 12. doi: 10.1021/acs.jmedchem.6c00456.

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