IPR-803
IPR-803 Basic information
- Product Name:
- IPR-803
- Synonyms:
-
- IPR-803
- Benzoic acid, 3-[[3-(hexahydro-1H-azepin-1-yl)-6-oxo-6H-anthra[1,9-cd]isoxazol-5-yl]amino]-
- inhibit,IPR 803,Inhibitor,IPR803,Threonine proteases,Serine proteases,IPR-803,Ser/Thr Protease,Serine endopeptidases
- IPR-803, 10 mM in DMSO
- CAS:
- 892243-35-5
- MF:
- C27H23N3O4
- MW:
- 453.49
- Mol File:
- 892243-35-5.mol
IPR-803 Chemical Properties
- Boiling point:
- 749.0±60.0 °C(Predicted)
- Density
- 1.401±0.06 g/cm3(Predicted)
- pka
- 4.17±0.10(Predicted)
- form
- Solid
- color
- Brown to reddish brown
IPR-803 Usage And Synthesis
Uses
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[1].
in vivo
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[1].
IPR-803 has a low oral bioavailability at 4 percent, and remains high concentration even after 10 hours in tumor tissue[1].
IPR-803 exhibits a half-life (t1/2) of 5 hours[1].
| Animal Model: | NSG mice with MDA-MB-231 cells xenograft[1] |
| 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[1] |
| Dosage: | 200 mg/kg (Pharmacokinetic Study) |
| Administration: | Oral administration |
| Result: | t1/2=5 hours. |
References
[1] Mani T, et al. Small-molecule inhibition of the uPARuPA interaction: synthesis, biochemical, cellular, in vivo pharmacokinetics and efficacy studies in breast cancer metastasis. Bioorg Med Chem. 2013 Apr 1;21(7):2145-55. DOI:10.1016/j.bmc.2012.12.047
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