2. Protein Tyrosine Kinase/RTK
  3. Ephrin Receptor PDGFR VEGFR
  4. JI-101

JI-101 

Cat. No.: HY-16265 Purity: 99.43%
COA Handling Instructions

JI-101 is an orally available multi-kinase inhibitor of VEGFR2, PDGFRβ and EphB4 with potent anti-cancer activity.

For research use only. We do not sell to patients.

JI-101 Chemical Structure

JI-101 Chemical Structure

CAS No. : 900573-88-8

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Solid + Solvent
10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 99 In-stock
Solid
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10 mg USD 160 In-stock
50 mg USD 550 In-stock
100 mg USD 950 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

JI-101 Related Antibodies

Top Publications Citing Use of Products

View All PDGFR Isoform Specific Products:

View All Isoforms
PDGFR PDGFRβ PDGFRα

View All VEGFR Isoform Specific Products:

View All Isoforms
VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

JI-101 is an orally available multi-kinase inhibitor of VEGFR2, PDGFRβ and EphB4 with potent anti-cancer activity.

IC50 & Target[1]

VEGFR2

 

PDGFRβ

 

In Vitro

JI-101 is found to be stable in all preclinical and human liver microsomes. The % metabolized is ranged between 3.03-3.95 across the tested species liver microsomes. The % metabolized is relatively higher in mice liver microsomes followed by dog, human and rat liver microsomes[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

JI-101 Related Antibodies
In Vivo

JI-101excreted through bile along with its mono- and di-hydroxy metabolites. Following oral administration, 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. Overall, the oral bioavailability of JI-101 is 55% and the primary route of elimination for JI-101 is feces[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

466.33

Appearance

Solid

Formula

C22H20BrN5O2
CAS No.
SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (214.44 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1444 mL 10.7220 mL 21.4440 mL
5 mM 0.4289 mL 2.1444 mL 4.2888 mL
10 mM 0.2144 mL 1.0722 mL 2.1444 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.36 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (5.36 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (5.36 mM); Clear solution

*All of the co-solvents are available by MedChemExpress (MCE).
Purity & Documentation
References
Animal Administration
[1]

Rats: Pharmacokinetics and bioavailability assessment of JI-101 are evaluated in a preliminary parallel-group study in male S.D. rats. Four rats (195–210 g) per route receive JI-101 at a dose of 3 and 30 mg/kg for i. v. (via tail vein) and oral dose (by gavage), respectively. Serial blood samples (100 μL) are collected from retro-orbital plexus at pre-dose, 0.12 ( i. v. only) 0.25, 0.5, 1, 2, 4, 8, 10 (oral only) and 24 h. Blood samples are collected in tubes containing K2 EDTA as the anticoagulant and centrifuged for 5 min maintained at 4 °C for plasma separation and stored frozen at −80±10 °C until analysis[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References
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JI-101 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

JI-101900573-88-8JI101JI 101Ephrin ReceptorPDGFRVEGFRPlatelet-derived growth factor receptorVascular endothelial growth factor receptorInhibitorinhibitorinhibit

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