IPR-803

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

IPR-803 是一种有效的 uPAR·uPA 蛋白-蛋白相互作用 (PPI) 抑制剂，具有抗肿瘤活性。 IPR-803 直接与 uPAR 结合，Ki 为 0.2 μM。

IPR-803 is an effective inhibitor of the uPAR·uPA protein-protein interaction (PPI) with anti-tumor activity. IPR-803 binds directly to uPAR with a Ki of 0.2 μM.(In Vitro):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 the cytotoxicity of the compound. IPR-803 (50 μM; 30 minutes) shows inhibition of MAPK phosphorylation. IPR-803 blocks invasion of breast cancer cells line MDA-MB-231, and inhibits matrix metalloproteinase breakdown of the extracellular matrix. IPR-803 impairs MDA-MB-231 cell adhesion and migration. IPR-803 induces a concentration-dependent impairment of cell adhesion with an IC50 of 30 μM. IPR-803 inhibits MDA-MB-231 cells growth with an IC50 of 58 μM.(In Vivo):In NSG mice with MDA-MB-231 cells xenograft, IPR-803 (200 mg/kg; i.g.; three times a week; for 5 weeks) impairs breast cancer metastasis with a t1/2 of 5 hours. IPR-803 has a low oral bioavailability at 4 percent, and remains high concentration even after 10 hours in tumor tissue.

Cell Proliferation Assay Cell Line:MDA-MB-231 cells Concentration:0 μM, 50 μM, 150 μM, 200 μM Incubation Time:3 days Result:Displays 90 percent blockage of invasion that is observed at 50 μM.

Animal Model:NSG mice with MDA-MB-231 cells xenograft Dosage:200 mg/kg Administration:Oral gavage; three times a week; for 5 weeks Result:Impaired metastasis to the lungs.Animal Model:NOD/SCID mice Dosage:200 mg/kg (Pharmacokinetic Study) Administration:Oral administration Result:t1/2=5 hours.

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Apoptosis

Serine/threonin kinase

Ca(2+) receptor

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892243-35-5

453.498

C27H23N3O4

>98% (HPLC)

In Vitro:?DMSO : 7.69 mg/mL (16.96 mM)

OC(=O)c1cccc(Nc2cc(N3CCCCCC3)c3noc4-c5ccccc5C(=O)c2c34)c1

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(-20℃)

With Ice Pack

≥ 2 years