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

JI-101 

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

JI-101 is an orally available multi-kinase inhibitor of VEGFR2PDGFRβ 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

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 172 In-stock
Estimated Time of Arrival: December 31
5 mg USD 156 In-stock
Estimated Time of Arrival: December 31
10 mg USD 228 In-stock
Estimated Time of Arrival: December 31
50 mg USD 792 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1320 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

View All PDGFR Isoform Specific Products:

View All VEGFR Isoform Specific Products:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

JI-101 is an orally available multi-kinase inhibitor of VEGFR2PDGFRβ 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].

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].

Clinical Trial
Solvent & Solubility
In Vitro: 

10 mM in DMSO

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.
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
Molecular Weight

466.33

Formula

C₂₂H₂₀BrN₅O₂

CAS No.

900573-88-8

SMILES

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

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

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

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

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number *

 

Organization name *

Country or Region *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
JI-101
Cat. No.:
HY-16265
Quantity:

JI-101

Cat. No.: HY-16265