IPR-803 是一种有效的 uPAR•uPA 蛋白-蛋白相互作用 (PPI) 抑制剂。IPR-803 直接与 uPAR 绑定，具有亚微摩尔的亲和力。IPR-803 具有抗肿瘤活性。

IPR-803 is a potent inhibitor of the uPAR?uPA protein-protein interaction (PPI). IPR-803 binds directly to uPAR with sub-micromolar affinity. IPR-803 displays anti-tumor activity.

Solid

Ki: 0.2 μM (PPI)

IPR-803 blocks invasion of breast cancer cells line MDA-MB-231, and inhibits matrix metalloproteinase (MMP) breakdown of the extracellular matrix (ECM).
IPR-803 impairs MDA-MB-231 cell adhesion and migration.
IPR-803 induces a concentration-dependent impairment of cell adhesion with an IC50 of approximately 30 μM.
IPR-803 inhibits MDA-MB-231 cells growth with an IC50 of 58 μM.
IPR-803 (0-200 μM; 3 days) blocks the invasion of MDA-MB-231 cells, and most of the inhibition of cell invasion is unlikely due to cytotoxicity of the compound.
IPR-803 (1-50 μM; 24 hours) does not have a significant effect on apoptosis or necrosis.
IPR-803 (50 μM; 30 minutes) shows inhibition of MAPK phosphorylation.
has not independently confirmed the accuracy of these methods. They are for refer

IPR-803 (200 mg/kg; i.g.; three times a week; for 5 weeks) impairs breast cancer metastasis, but no statistical significance to the differences in body weight between treated and untreated.
IPR-803 has a low oral bioavailability at 4 percent, and remains high concentration even after 10 hours in tumor tissue.
IPR-803 exhibits a half-life (t1/2) of 5 hours.
has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Mani T, et al. Small-molecule inhibition of the uPAR?uPA interaction: synthesis, biochemical, cellular, in vivo pharmacokinetics and efficacy studies in breast cancer metastasis. Bioorg Med Chem. 2013 Apr 1;21(7):2145-55.

In Vitro: DMSO : 7.69 mg/mL (16.96 mM; Need ultrasonic)配制储备液