JI-101

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WARNING: This product is for research use only, not for human or veterinary use.

Description: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.

Price and Availability

JI-101, purity > 98%, is in stock. Minimum order of 100mg.Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.

Chemical Structure

Theoretical Analysis

MedKoo Cat#: 201611Name: JI-101CAS#: 900573-88-8Chemical Formula: C22H20BrN5O2Exact Mass: 465.08004Molecular Weight: 466.3305Elemental Analysis:C, 56.66; H, 4.32; Br, 17.13; N, 15.02; O, 6.86

Synonym:JI101, JI 101, JI-101

IUPAC/Chemical Name:1-(1-((2-aminopyridin-4-yl)methyl)-1H-indol-4-yl)-3-(5-bromo-2-methoxyphenyl)urea.

InChi Key:ZXBFYBLSJMEBEP-UHFFFAOYSA-N

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)

SMILES Code:O=C(NC1=CC(Br)=CC=C1OC)NC2=CC=CC3=C2C=CN3CC4=CC(N)=NC=C4

Technical Data

Additional Information

JI-101 is a novel orally active kinase inhibitor, which has shown potent in vitro and in vivo anticancer activity against a variety of cancer cell lines and xenografts. It is currently entering Phase II clinical development for the treatment of solid tumors. Overall, the oral bioavailability of JI-101 is 55% and the primary route of elimination for JI-101 is feces.  (source: Arzneimittelforschung. 2012 Jan;62(1):27-34. Epub 2012 Jan 10.)    

References

1: Gurav SD, Gilibili RR, Jeniffer S, Mohd Z, Giri S,Govindarajan R, Srinivas NR, Mullangi R. Pharmacokinetics, tissuedistribution and identification of putative metabolites of JI-101 - anovel triple kinase inhibitor in rats. Arzneimittelforschung. 2012Jan;62(1):27-34. Epub 2012 Jan 10. PubMed PMID: 22331760.

2: Gurav SD, Jeniffer S, Punde R, Gilibili RR, Giri S, Srinivas NR,Mullangi R. A strategy for extending the applicability of a validatedplasma calibration curve to quantitative measurements in multiple tissuehomogenate samples: a case study from a rat tissue distribution study ofJI-101, a triple kinase inhibitor. Biomed Chromatogr. 2012Apr;26(4):419-24. doi: 10.1002/bmc.1680. Epub 2011 Aug 23. PubMed PMID:21877323.

3: Sharma S, Dubey NK, Dasgupta AK, Sahu M, Benjamin B, Mullangi R,Srinivas NR. Highly sensitive method for the determination of JI-101, amulti-kinase inhibitor in human plasma and urine by LC-MS/MS-ESI: methodvalidation and application to a clinical pharmacokinetic study. BiomedChromatogr. 2012 Feb;26(2):232-8. doi: 10.1002/bmc.1652. Epub 2011 May19. PubMed PMID: 21594880.

4: Gurav SD, Gilibili RR, Jeniffer S, Giri S, Srinivas NR, Mullangi R.Highly sensitive method for the determination of a novel triple kinaseinhibitor with anti-cancer activity, JI-101, in rat plasma by liquidchromatography-electrospray ionization tandem mass spectrometry:application to a pharmacokinetic study. Biomed Chromatogr. 2011Jul;25(7):794-800. doi: 10.1002/bmc.1518. Epub 2010 Sep 27. PubMed PMID:20872957.

(Last updated: 4/20/2016).