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.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.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.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.JI-101 hydrochloride can be used for the research of ovarian cancer and solid tumors.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 2514957-81-2
- 分子式: C22H21BrClN5O2
- 分子量:502.79
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
VEGFR アイソフォーム固有の製品をすべて表示
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生物活性
製品説明
IC50 & Target
[1]|
EPHB4 |
VEGFR2 |
PDGFR-β |
体外実験
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.
Parmacokinetics
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 2514957-81-2
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分子量 502.79
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分子式 C22H21BrClN5O2
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SMILES
O=C(NC1=CC(Br)=CC=C1OC)NC2=CC=CC3=C2C=CN3CC4=CC(N)=NC=C4.Cl
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[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]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)