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JI-101

Cat. No. M8949
JI-101 Structure
Size Price Availability
10mg USD 240 4-7 Days
25mg USD 440 4-7 Days
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

JI-101 is an orally available multi-kinase inhibitor of VEGFR2,PDGFRβ and EphB4 with potent anti-cancer activity. JI-101 is rapidly absorbed, reaching Cmax within 2 h. The t1/2 of JI-101 with intravenous and oral route is found to be 1.75±0.79 and 2.66±0.13 h, respectively. The Cl and Vd by intravenous route for JI-101 are found to be 13.0±2.62 mL/min/kg and 2.11±1.42 L/kg, respectively. The tissue distribution of JI-101 is extensive with rapid and preferred uptake into lung tissue.

Protocol
Cell Experiment
Cell lines
Preparation method
Concentrations
Incubation time
Animal Experiment
Animal models male S.D. rats
Formulation
Dosages 3 and 30 mg/kg
Administration i. v. (via tail vein) and oral dose (by gavage)
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 466.33
Formula C22H20BrN5O2
CAS Number 900573-88-8
Purity >98%
Solubility DMSO 10 mM
Storage at -20°C
References

Pharmacokinetics, tissue distribution and identification of putative metabolites of JI-101 - a novel triple kinase inhibitor in rats.
Gurav SD, et al. Arzneimittelforschung. 2012 Jan;62(1):27-34. PMID: 22331760.

Highly sensitive method for the determination of JI-101, a multi-kinase inhibitor in human plasma and urine by LC-MS/MS-ESI: method validation and application to a clinical pharmacokinetic study.
Sharma S, et al. Biomed Chromatogr. 2012 Feb;26(2):232-8. PMID: 21594880.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: JI-101 supplier, VEGFR/PDGFR, inhibitors

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