JI-101 hydrochloride 

JI-101 hydrochloride is an orally active angiogenesis inhibitor and anticancer agent with 55% oral bioavailability in Sprague Dawley rats, high permeability, and no P-gp substrate activity^[1][2].JI-101 hydrochloride modulates angiogenesis signaling pathways in tumor vessel beds, downregulates EphB4, targets EphB4, VEGFR-2, and PDGFR-β, and inhibits multiple stages of tumor angiogenesis^[1].JI-101 hydrochloride exerts activity against cancer cells and xenografts, exhibits mild to moderate inhibition of CYP3A4, and shows stability in pre-clinical and human liver microsomes^[1][2].JI-101 hydrochloride undergoes rapid oral absorption in Sprague Dawley rats, has extensive tissue distribution with preferred lung uptake, and is excreted via bile with mono- and di-hydroxy metabolites, with feces as the primary elimination route^[2].JI-101 hydrochloride can be used for the research of ovarian cancer and solid tumors^[1][2].

JI-101 (10 μM; 0-30 min) hydrochloride exhibits high stability in mouse, rat, dog and human liver microsomes, with only 3.03-3.95% metabolism observed after 30 min of incubation^[2].
JI-101 (1 μM; 15 min) hydrochloride is mainly metabolized by recombinant human CYP1A1 (with ~44% activity reduction) and CYP3A4 (with 10% activity reduction)^[2].
JI-101 (10-100 μM; 0-120 min) hydrochloride efficiently penetrates the Caco-2 cell monolayer, with an efflux ratio of 0.32^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

JI-101 (1-3 mg/kg; i.v. via tail vein; single dose; 10-30 mg/kg; p.o. by gavage; single dose) demonstrates 54.7% oral bioavailability in male Sprague Dawley rats, with preferential and persistent uptake in lung tissue^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

502.79

C₂₂H₂₁BrClN₅O₂

2514957-81-2

O=C(NC1=CC(Br)=CC=C1OC)NC2=CC=CC3=C2C=CN3CC4=CC(N)=NC=C4.Cl

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Werner TL, et al. A pilot study of JI-101, an inhibitor of VEGFR-2, PDGFR-β, and EphB4 receptors, in combination with everolimus and as a single agent in an ovarian cancer expansion cohort. Invest New Drugs. 2015;33(6):1217-1224.  [Content Brief]

  [2]. Gurav SD, et al. Pharmacokinetics, tissue distribution and identification of putative metabolites of JI-101 - a novel triple kinase inhibitor in rats. Arzneimittelforschung. 2012;62(1):27-34.  [Content Brief]