PHGDH-IN-3_product_DataBase

Bioactivity	PHGDH-IN-3 is an orally active phosphoglycerate dehydrogenase (PHGDH) inhibitor. PHGDH-IN-3 inhibits PHGDH with an IC50 value of 2.8 μM. PHGDH-IN-3 can be used for the research of cancer[1].
Target	IC50: 2.8 μM (PHGDH).Kd: 2.33 μM (PHGDH)
Invitro	PHGDH-IN-3 (compound D8) 具有良好的酶促抑制活性，IC50 值为 2.8 μM[1]。PHGDH-IN-3 对 PHGDH 蛋白具有高结合亲和力，Kd 值为2.33 μM[1]。PHGDH-IN-3 对 PHGDH 基因扩增或过表达的细胞株具有敏感性[1]。PHGDH-IN-3 可以限制 MDA-MB-468 细胞内葡萄糖从头合成丝氨酸[1]。
In Vivo	PHGDH-IN-3 (compound D8) (p.o., i.v.; 1, 3 mg/kg) 表现出优异的体内药代动力学特性[1]。PHGDH-IN-3（i.p.；12.5、25、50 mg/kg；每天一次，连续 31 天）在 PC9 异种移植小鼠模型中发挥明显的抗肿瘤作用[1]。 Animal Model:
Name	PHGDH-IN-3
CAS	2893778-31-7
Formula	C24H18FN3O4S2
Molar Mass	495.55
Appearance	Solid
Transport	Room temperature in continental US; may vary elsewhere.
Storage	4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Reference	[1]. Dingding Gao, et al. Discovery of Novel Drug-like PHGDH Inhibitors to Disrupt Serine Biosynthesis for Cancer Therapy. J Med Chem. 2023 Jan 12;66(1):285-305.

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