PHGDH-IN-3

PHGDH-IN-3 is an orally active phosphoglycerate dehydrogenase (PHGDH) inhibitor. PHGDH-IN-3 inhibits PHGDH with an IC 50 value of 2.8 μM. PHGDH-IN-3 can be used for the research of cancer In Vitro PHGDH-IN-3 (compound D8) has good enzymatic inhibitory activity with an IC 50 value of 2.8 μM. PHGDH-IN-3 has high binding affinity for the PHGDH protein with a K d value of 2.33 μM. PHGDH-IN-3 has sensitivity to the cell lines with the PHGDH gene amplification or overexpression. PHGDH-IN-3 can restrict the de novo serine synthesis from glucose within MDA-MB-468 cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo PHGDH-IN-3 (compound D8) (p.o., i.v.; 1, 3 mg/kg) exhibits excellent in vivo pharmacokinetic properties . PHGDH-IN-3 (i.p.; 12.5, 25, 50 mg/kg; once daily for consecutive 31 days) exertes evident antitumor efficacy in the PC9 xenograft mouse model . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: ICR mice 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 (h•ng/mL) 38,358 ± 14,768 94,386 ± 23,416 T 1/2 (h) 4.94 ± 0.38 4.74 ± 0.30 T max (h) 3.33 ± 1.15 CL _obs (mL/min/kg) 0.48 ± 0.23 C max (ng/mL) 8842 ± 1755 F (%) 82.0 Animal Model: Balb/c nude mice 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. Form:Solid IC50& Target:IC50: 2.8 μM (PHGDH),Kd: 2.33 μM (PHGDH)

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