| Bioactivity | PKUMDL-WQ-2101 is a non-NAD+-competing allosteric phosphoglycerate dehydrogenase (PHGDH) inhibitor with an IC50 of 34.8 μM. PKUMDL-WQ-2101 exhibits antitumor activity[1]. | |||||||||
| Target | IC50: 34.8 μM (PHGDH) | |||||||||
| Invitro | PKUMDL-WQ-2101（72 小时）在微摩尔浓度下显示出对细胞活力的剂量依赖性抑制作用，对 PHGDH 扩增的乳腺癌细胞系具有良好的选择性。PKUMDL-WQ-2101 在两种 PHGDH 扩增的乳腺癌细胞系（MDA-MB-468 和 HCC70）中的抗肿瘤活性分别为 7.70 μM 和 10.8 μM[1]。PKUMDL-WQ-2101（2.5-40 μM；24 小时）导致 MDA-MB-468 细胞的细胞周期停滞[1]。PKUMDL-WQ-2101（37 μM；24 小时）减少丝氨酸合成途径下游的丝氨酸从头合成和代谢，其作用与 PHGDH 基因缺失相当[1]。 Cell Viability Assay[1] Cell Line: | |||||||||
| In Vivo | PKUMDL-WQ-2101（5-20 mg/kg；i.p；每天；持续 30 天）对 MDA-MB-468 异种移植物表现出显着的抑制作用[1]。 Animal Model: | |||||||||
| Name | PKUMDL-WQ-2101 | |||||||||
| CAS | 304481-72-9 | |||||||||
| Formula | C14H11N3O6 | |||||||||
| Molar Mass | 317.25 | |||||||||
| Appearance | Solid | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
| Storage |
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| Reference | [1]. Qian Wang, 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. |
PKUMDL-WQ-2101
CAS: 304481-72-9 F: C14H11N3O6 W: 317.25
PKUMDL-WQ-2101 is a non-NAD+-competing allosteric phosphoglycerate dehydrogenase (PHGDH) inhibitor with an IC50 of 34.8
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