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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.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $84 | In Stock | |
5 mg | $197 | In Stock | |
10 mg | $328 | In Stock | |
25 mg | $558 | In Stock | |
50 mg | $788 | In Stock | |
1 mL x 10 mM (in DMSO) | $226 | In Stock |
Description | 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. |
Targets&IC50 | PPI:ki: 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[1]. |
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[1]. |
Molecular Weight | 453.49 |
Formula | C27H23N3O4 |
Cas No. | 892243-35-5 |
Smiles | OC(=O)c1cccc(Nc2cc(N3CCCCCC3)c3noc4-c5ccccc5C(=O)c2c34)c1 |
Relative Density. | 1.401 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||
Solubility Information | DMSO: 7 mg/mL (15.44 mM), Sonication is recommended. | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
DMSO
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