IPR-803

IPR-803CAS号: 892243-35-5分子式: C27H23N3O4分子量: 453.49描述纯度储存/保存方法可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)

产品描述
描述
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.
纯度
95%
储存/保存方法
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
基本信息
可溶性/溶解性
DMSO:7 mg/mL (15.44 mM)
生物活性
靶点
PPI(ki):ki: 0.2 μM
In vitro(体外研究)
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(体内研究)
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].