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 在小鼠、大鼠、犬和人肝微粒体中表现出高稳定性，孵育 30 min 后仅代谢 3.03-3.95%^[2]。
JI-101 (1 μM; 15 min) hydrochloride 主要经重组人 CYP1A1 (活性下降 ~44%) 和 CYP3A4 (活性下降 10%) 代谢^[2]。
JI-101 (10-100 μM; 0-120 min) hydrochloride 可高效穿透 Caco-2 细胞单层，其外排率为 0.32^[2]。

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

JI-101 (1-3 mg/kg；尾静脉注射；10-30 mg/kg；口服) 在雄性 Sprague Dawley 大鼠中表现出 54.7% 的口服生物利用度，其在肺组织中存在优先且持续的摄取^[2]。

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

502.79

C₂₂H₂₁BrClN₅O₂

2514957-81-2

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]