JI-101

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

JI-101是一种口服多激酶抑制剂，靶向血管内皮生长因子受体2型（VEGFR-2）、血小板衍生生长因子受体β（PDGFR-β）和肝配蛋白B型受体4（EphB4）。

JI-101 is an orally active inhibitor of vascular endothelial growth factor receptor 2 (VEGFR2), platelet-derived growth factor receptor beta (PDGFRb), and the ephrin B4 receptor B4 (EphB4) with potential antiangiogenic and antineoplastic activities. Angiogenesis inhibitor JI-101 binds to and inhibits VEGFR2, PDGFRb and EphB4, which may inhibit tumor angiogenesis and, so, cellular proliferation in tumor cells overexpressing VEGFR2, PDGFRb and EphB4. The receptor tyrosine kinases VEGFR2, PDGFRb and EphB4 may be overexpressed in a number of different cancer cell types and may play crucial roles in tumor angiogenesis.(In Vitro):JI-101 is found to be stable in all preclinical and human liver microsomes. The % metabolized is ranged between 3.03-3.95 across the tested species liver microsomes. The % metabolized is relatively higher in mice liver microsomes followed by dog, human and rat liver microsomes.(In Vivo):JI-101excreted through bile along with its mono- and di-hydroxy metabolites. Following oral administration, JI-101 is rapidly absorbed, reaching Cmax within 2?h. The t1/2 of JI-101 with intravenous and oral route is found to be 1.75±0.79 and 2.66±0.13?h, respectively. The Cl and Vd by intravenous route for JI-101 are found to be 13.0±2.62?mL/min/kg and 2.11±1.42?L/kg, respectively. The tissue distribution of JI-101 is extensive with rapid and preferred uptake into lung tissue. Overall, the oral bioavailability of JI-101 is 55% and the primary route of elimination for JI-101 is feces.

JI-101 is found to be stable in all preclinical and human liver microsomes. The % metabolized is ranged between 3.03-3.95 across the tested species liver microsomes. The % metabolized is relatively higher in mice liver microsomes followed by dog, human and rat liver microsomes.

JI-101excreted through bile along with its mono- and di-hydroxy metabolites. Following oral administration, JI-101 is rapidly absorbed, reaching Cmax within 2?h. The t1/2 of JI-101 with intravenous and oral route is found to be 1.75±0.79 and 2.66±0.13?h, respectively. The Cl and Vd by intravenous route for JI-101 are found to be 13.0±2.62?mL/min/kg and 2.11±1.42?L/kg, respectively. The tissue distribution of JI-101 is extensive with rapid and preferred uptake into lung tissue. Overall, the oral bioavailability of JI-101 is 55% and the primary route of elimination for JI-101 is feces.

JI101, JI 101, JI-101

Others

Other Targets

Ephrin Receptor| PDGFR| VEGFR

Cardiovascular Disease

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900573-88-8

466.34

C22H20BrN5O2

>98% (HPLC)

DMSO : ≥ 100 mg/mL; 214.44 mM

N(C(=O)Nc1c(ccc(c1)Br)OC)c1c2ccn(c2ccc1)Cc1cc(ncc1)N

1-(1-((2-aminopyridin-4-yl)methyl)-1H-indol-4-yl)-3-(5-bromo-2-methoxyphenyl)urea.

(-20℃)

With Ice Pack

≥ 2 years