PKUMDL-WQ-2201 是一种 PHGDH 非 NAD+ 竞争变构抑制剂 | MedChemExpress (MCE)

PKUMDL-WQ-2201

CAS：592474-91-4

品牌：MedChemExpress (MCE)

存储条件：Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month

生物活性：PKUMDL-WQ-2201 是一种 PHGDH 非 NAD+ 竞争变构抑制剂 (IC50=35.7 μM)。PKUMDL-WQ-2201 对 PHGDH 突变体的 IC50 分别为 69 μM (T59A) 和300 μM (T56AK57A)。PKUMDL-WQ-2201 抑制癌细胞中丝氨酸的从头合成，并减少肿瘤生长。

体外：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]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内：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]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献：

[1]. 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.
[2]. 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.