MedKoo Biosciences

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

JI-101

CAS# 900573-88-8

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 201611
Name: JI-101
CAS#: 900573-88-8
Chemical Formula: C22H20BrN5O2
Exact Mass: 465.08
Molecular Weight: 466.339
Elemental Analysis: C, 56.66; H, 4.32; Br, 17.13; N, 15.02; O, 6.86

Price and Availability

Size	Price	Availability
25mg	USD 250	2 Weeks
50mg	USD 450	2 Weeks
100mg	USD 750	2 Weeks
200mg	USD 1250	2 Weeks
500mg	USD 2650	2 Weeks
1g	USD 3850	2 Weeks
2g	USD 6450	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

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

Product Data:

Product Data

Instruction:

View handling instruction

Biological target:	JI-101 is an orally available multi-kinase inhibitor of VEGFR2, PDGFRβ and EphB4 with potent anti-cancer activity.
In vitro activity:	The treatment with 10 µM of JI‐101 also decreased the proliferation rate of EPHB4 mutant clone compared to vehicle (DMSO) in SHSY5Y cells, and also of EPHB4‐WT compared to vehicle (Figure 6B) at 72 hours. Reference: J Cell Mol Med. 2020 Jun;24(11):6459-6471. https://pubmed.ncbi.nlm.nih.gov/32336043/
In vivo activity:	TBD

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	100.0	214.44

Preparing Stock Solutions

The following data is based on the product molecular weight 466.339000000000000000000000000000 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.

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

Formulation protocol:	1. Andolfo I, Lasorsa VA, Manna F, Rosato BE, Formicola D, Iolascon A, Capasso M. Kinome multigenic panel identified novel druggable EPHB4-V871I somatic variant in high-risk neuroblastoma. J Cell Mol Med. 2020 Jun;24(11):6459-6471. doi: 10.1111/jcmm.15297. Epub 2020 Apr 26. PMID: 32336043; PMCID: PMC7294133.
In vitro protocol:	1. Andolfo I, Lasorsa VA, Manna F, Rosato BE, Formicola D, Iolascon A, Capasso M. Kinome multigenic panel identified novel druggable EPHB4-V871I somatic variant in high-risk neuroblastoma. J Cell Mol Med. 2020 Jun;24(11):6459-6471. doi: 10.1111/jcmm.15297. Epub 2020 Apr 26. PMID: 32336043; PMCID: PMC7294133.
In vivo protocol:	TBD

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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).

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