1. Protein Tyrosine Kinase/RTK
  2. Ephrin Receptor
    PDGFR
    VEGFR

JI-101 (Synonyms: JI 101; JI101)

Cat. No.: HY-16265 Purity: 99.78%
Data Sheet SDS Handling Instructions

JI-101 is an oral multi-kinase inhibitor that targets vascular endothelial growth factor receptor type 2 (VEGFR-2), platelet derived growth factor receptor β (PDGFR-β), and ephrin type-B receptor 4 (EphB4). JI-101 inhibits angiogenesis, and subsequently tumor growth. [1]

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JI-101 Chemical Structure

JI-101 Chemical Structure

CAS No. : 900573-88-8

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $143 In-stock
5 mg $130 In-stock
10 mg $190 In-stock
50 mg $660 In-stock
100 mg $1100 In-stock
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500 mg   Get quote  

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Description

JI-101 is an oral multi-kinase inhibitor that targets vascular endothelial growth factor receptor type 2 (VEGFR-2), platelet derived growth factor receptor β (PDGFR-β), and ephrin type-B receptor 4 (EphB4). JI-101 inhibits angiogenesis, and subsequently tumor growth. [1] In vitro :Caco-2 human intestinal epithelial cells were plated in 24-Transwell dual chamber plates (cell density of 500 000 cells/cm2 on day-1). The permeability studies were conducted with the monolayers cultured for 20-23 days in culture. The integrity of each Caco-2 cell monolayer was certified by trans-epithelial electrical resistance (TEER) test (pre-experiment) and by determining the permeability of reference compounds3H-propranolol (high permeability) and 3H-mannitol (low permeability). In addition, the reference substrate 3H-vinblastine was included as a positive control P-gp substrate. The concentration of JI-101 used in the assay was 10 and 100 uM. All the stocks were made in DMSO and the final concentration of DMSO in spiking solution was 0.5%. [2] in vivo: For oral administration JI-101 was formulated as a suspension with 20 μL of Tween-80 and 0.5% methyl cellulose. Pharmacokinetics and bioavailability assessment of JI-101 were evaluated in a preliminary parallel-group study in male S.D. rats. Four rats (195-210 g) per route received JI-101 at a dose of 3 and 30 mg/kg for i.v. (via tail vein) and oral dose (by gavage), respectively.[2]

References
M.Wt

466.33

Formula

C₂₂H₂₀BrN₅O₂

CAS No.

900573-88-8

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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JI-101
Cat. No.:
HY-16265
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