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 (h•ng/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 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
In Vitro
PHGDH-IN-3 (compound D8) exhibits potent enzyme inhibition with an IC50 value of 2.8 μM [1]. It demonstrates high binding affinity to the PHGDH protein with a Kd value of 2.33 μM [1]. PHGDH-IN-3 shows sensitivity towards cell lines with PHGDH gene amplification or overexpression [1]. Additionally, it can limit de novo serine synthesis from glucose in MDA-MB-468 cells [1].
Kinase Assay
Cell Assay
Animal Administration
References
[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.
Return Policy
If you are in any way unsatisfied with your purchase, you may return any item(s) within 365 days of its original purchase date.
Please provide your Order Number in the email. We strive to reply to all email inquiries within one business day.
