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JI-101

Cat. No. M8949
JI-101 Structure
Size Price Availability Quantity
5mg USD 85  USD85 In stock
10mg USD 140  USD140 In stock
25mg USD 280  USD280 In stock
50mg USD 480  USD480 In stock
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Quality Control & Documentation
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 (for reference only)
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)
Chemical Information
Molecular Weight 466.33
Formula C22H20BrN5O2
CAS Number 900573-88-8
Solubility (25°C) DMSO 10 mM
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Gurav SD, et al. Arzneimittelforschung. Pharmacokinetics, tissue distribution and identification of putative metabolites of JI-101 - a novel triple kinase inhibitor in rats.

[2] Sharma S, et al. Biomed Chromatogr. 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.

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


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