| Bioactivity | 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[1][2]. | ||||||||||||
| Target | IC50: 35.7 μM (PHGDH WT), 69 μM (PHGDH T59A), >300 μM (PHGDH T56AK57A) | ||||||||||||
| Invitro | 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]。 | ||||||||||||
| In Vivo | 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]。 | ||||||||||||
| Name | PKUMDL-WQ-2201 | ||||||||||||
| CAS | 592474-91-4 | ||||||||||||
| Formula | C15H14ClN3O3S | ||||||||||||
| Molar Mass | 351.81 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
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| Reference | [1]. 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. [2]. 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. |
PKUMDL-WQ-2201
CAS: 592474-91-4 F: C15H14ClN3O3S W: 351.81
PKUMDL-WQ-2201 is a PHGDH non-NAD+-competing allosteric inhibitor (IC50=35.7 μM). PKUMDL-WQ-2201 also inhibits PHGDH mu
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