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Purity: ≥98%
JI-101 is an orally bioactive multi-kinase 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. JI-101 has demonstrated strong anticancer activity against a range of cancer cell lines and xenografts both in vitro and in vivo. For the treatment of solid tumors, it is presently in Phase II clinical development. In all preclinical and human liver microsomes, JI-101 is found to be stable. Across the tested species of liver microsomes, the percentage metabolized ranges from 3.03 to 3.95. Rat, dog, and human liver microsomes are the next in order of percentage metabolized, which is comparatively higher in mice liver microsomes.
| Targets |
VEGFR2; PDGFRβ
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| ln Vitro |
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| ln Vivo |
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| Enzyme Assay |
JI-101 is an oral bioactive multi-kinase inhibitor that has the ability to inhibit the activities of platelet-derived growth factor receptor beta (PDGFRb), vascular endothelial growth factor receptor 2 (VEGFR2), and ephrin B4 receptor B4 (EphB4). It may also have antiangiogenic and antineoplastic properties.
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| Cell Assay |
It has been discovered that JI-101 is stable in both human and preclinical liver microsomes. The percentage of metabolized liver microsomes in the tested species ranges from 3.03 to 3.95. Mice liver microsomes have a comparatively higher percentage of metabolized material compared to dog, human, and rat liver microsomes.
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| Animal Protocol |
Rats: In a preliminary parallel-group study, male S.D. rats are used to assess the pharmacokinetics and bioavailability of JI-101. JI-101 is administered intravenously (IV) via tail vein to four rats weighing between 195 and 210 g, orally by gavage, at a dose of 30 mg/kg. At pre-dose, 0.12 (i.v. only), 0.25, 0.5, 1, 2, 4, 8, 10 (oral only), and 24 hours, serial blood samples (100 μL) are taken from the retro-orbital plexus. Samples of blood are taken in tubes with K2 EDTA as the anticoagulant, centrifuged for 5 minutes at 4 °C to separate the plasma, and then frozen at -80±10 °C until analysis[1].
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| References | ||
| Additional Infomation |
JI-101 has been used in trials studying the treatment of Cancer, Colon Cancer, Neuroendocrine, Ovarian Cancer, and Advanced Solid Tumors.
Angiogenesis Inhibitor 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. |
| Molecular Formula |
C₂₂H₂₀BRN₅O₂
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| Molecular Weight |
466.33
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| Exact Mass |
465.08
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| Elemental Analysis |
C, 56.66; H, 4.32; Br, 17.13; N, 15.02; O, 6.86
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| CAS # |
900573-88-8
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| Related CAS # |
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| PubChem CID |
11691242
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| Appearance |
White to off-white solid powder
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| LogP |
5.098
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
30
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| Complexity |
582
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(NC1C(OC)=CC=C(Br)C=1)NC1C2C=CN(C=2C=CC=1)CC1C=C(N)N=CC=1
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| InChi Key |
ZXBFYBLSJMEBEP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H20BrN5O2/c1-30-20-6-5-15(23)12-18(20)27-22(29)26-17-3-2-4-19-16(17)8-10-28(19)13-14-7-9-25-21(24)11-14/h2-12H,13H2,1H3,(H2,24,25)(H2,26,27,29)
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| Chemical Name |
1-[1-[(2-aminopyridin-4-yl)methyl]indol-4-yl]-3-(5-bromo-2-methoxyphenyl)urea
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.36 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.36 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.36 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1444 mL | 10.7220 mL | 21.4440 mL | |
| 5 mM | 0.4289 mL | 2.1444 mL | 4.2888 mL | |
| 10 mM | 0.2144 mL | 1.0722 mL | 2.1444 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00842335 | Completed | Drug: JI-101 | Advanced Solid Tumors | Jubilant Innovation Ltd. | February 2009 | Phase 1 Phase 2 |
| NCT01149434 | Terminated | Drug: JI-101 Drug: Everolimus |
Cancer Neuroendocrine |
University of Utah | September 2010 | Phase 1 Phase 2 |
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