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.
For research use only. We do not sell to patients.
- CAS No.: 2514957-81-2
- Formula: C22H21BrClN5O2
- Molecular Weight:502.79
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All VEGFR Isoforms
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Biological Activity
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EPHB4 |
VEGFR2 |
PDGFR-β |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2514957-81-2
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Molecular Weight 502.79
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)