PHGDH-IN-3 is an orally activephosphoglycerate dehydrogenase (PHGDH)inhibitor. PHGDH-IN-3 inhibits PHGDH with anIC₅₀value of 2.8 μM. PHGDH-IN-3 can be used for the research ofcancer^[1].

IC50: 2.8 μM (PHGDH)^[1].
Kd: 2.33 μM (PHGDH)^[1]

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，K_d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]。

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:	ICR mice[1]
Dosage:	1, 3 mg/kg
Administration:	Oral (p.o.) and intravenous (i.v.) administration
Result:	PK parameters i.v. (1 mg/kg) p.o. (3 mg/kg) AUC (hong/mL) 38,358 ± 14,768 94,386 ± 23,416 T1/2(h) 4.94 ± 0.38 4.74 ± 0.30 Tmax(h) 3.33 ± 1.15 CL_obs(mL/min/kg) 0.48 ± 0.23 Cmax(ng/mL) 8842 ± 1755 F (%) 82.0 map

Animal Model:	Balb/c nude mice[1]
Dosage:	12.5, 25, 50 mg/kg
Administration:	Intraperitoneal (i.p.); once daily for consecutive 31 days
Result:	Exhibited an in vivo anti-tumor effect and significantly delayed the tumor growth. Significantly abated the tumor weights of mice at 25 mg/ kg.

495.55

C₂₄H₁₈FN₃O₄S₂

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