PKUMDL-WQ-2201 is aPHGDHnon-NAD+-competing allosteric inhibitor (IC₅₀=35.7 μM). PKUMDL-WQ-2201 also inhibits PHGDH mutants withIC₅₀s of 69 μM (T59A) and >300 μM (T56AK57A), respectively. PKUMDL-WQ-2201 inhibits de novo serine synthesis incancercells, and reduces tumor growth^[1][2].

IC50: 35.7 μM (PHGDH WT), 69 μM (PHGDH T59A), >300 μM (PHGDH T56AK57A)^[1]

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)^[1]。

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^[1]。

351.81

C₁₅H₁₄ClN₃O₃S

592474-91-4

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.