JI-101
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 201611

CAS#: 900573-88-8

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.


Chemical Structure

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JI-101
CAS# 900573-88-8

Theoretical Analysis

MedKoo Cat#: 201611
Name: JI-101
CAS#: 900573-88-8
Chemical Formula: C22H20BrN5O2
Exact Mass: 465.08004
Molecular Weight: 466.3305
Elemental Analysis: C, 56.66; H, 4.32; Br, 17.13; N, 15.02; O, 6.86

Size Price Shipping out time Quantity
100mg USD 1450 2 Weeks
200mg USD 1850 2 Weeks
500mg USD 2450 2 Weeks
1g USD 3250 2 Weeks
2g USD 5250 2 Weeks
Inquire bulk and customized quantity

Pricing updated 2021-02-25. Prices are subject to change without notice.

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.

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

Appearance:
Solid powder

Purity:
>98%

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>5 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code:
2934.99.9001

Handling Instructions:

Preparing Stock Solutions

The following data is based on the product molecular weight 466.3305 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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1: Gurav SD, Gilibili RR, Jeniffer S, Mohd Z, Giri S, Govindarajan R, Srinivas NR, Mullangi R. Pharmacokinetics, tissue distribution and identification of putative metabolites of JI-101 - a novel triple kinase inhibitor in rats. Arzneimittelforschung. 2012 Jan;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 validated plasma calibration curve to quantitative measurements in multiple tissue homogenate samples: a case study from a rat tissue distribution study of JI-101, a triple kinase inhibitor. Biomed Chromatogr. 2012 Apr;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, a multi-kinase inhibitor in human plasma and urine by LC-MS/MS-ESI: method validation and application to a clinical pharmacokinetic study. Biomed Chromatogr. 2012 Feb;26(2):232-8. doi: 10.1002/bmc.1652. Epub 2011 May 19. 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 kinase inhibitor with anti-cancer activity, JI-101, in rat plasma by liquid chromatography-electrospray ionization tandem mass spectrometry: application to a pharmacokinetic study. Biomed Chromatogr. 2011 Jul;25(7):794-800. doi: 10.1002/bmc.1518. Epub 2010 Sep 27. PubMed PMID: 20872957.

(Last updated: 4/20/2016).

JI-101

10mg / Not available


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.)