PKUMDL-WQ-2201 is a PHGDH non-NAD+-competing allosteric inhibitor (IC₅₀=35.7 μM). PKUMDL-WQ-2201 also inhibits PHGDH mutants with IC₅₀s of 69 μM (T59A) and >300 μM (T56AK57A), respectively. PKUMDL-WQ-2201 inhibits de novo serine synthesis in cancer cells, and reduces tumor growth.

PKUMDL-WQ-2201 (10 nM-100 μM; 3 d) 对 PHGDH 扩增的乳腺癌细胞系具有良好的选择性和抑制作用，EC₅₀ 值分别为 7.7 μM (MDA-MB-468) 和 10.8 μM (HCC70)。

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

PKUMDL-WQ-2201 (5-20 mg/kg; 腹腔注射; 每天 1 次, 共 30 天) 与对照组小鼠相比，对 MDA-MB-468 异种移植有显著的抑制作用，但不影响肿瘤生长。

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

PKUMDL-WQ-2201 (5-20 mg/kg; 腹腔注射; 每天 1 次, 共 30 天) 与对照组小鼠相比，对 MDA-MB-468 异种移植有显著的抑制作用，但不影响肿瘤生长。

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

• . Wang Q, et al. Rational Design of Selective Allosteric Inhibitors of PHGDH and Serine Synthesis with Anti-tumor Activity. Cell Chem Biol. 2017 Jan 19;24(1):55-65.  [Content Brief]

  . Zhao JY, et al. A retrospective overview of PHGDH and its inhibitors for regulating cancer metabolism. Eur J Med Chem. 2021 May 5;217:113379.  [Content Brief]