Referencia número: HY-16265

JI-101

Revisión del cliente

Based on 1 Customer Validation

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

Para uso exclusivo en investigación. No vendemos a pacientes.

Pureza: 98.99%
No. CAS: 900573-88-8
Fòrmula: C₂₂H₂₀BrN₅O₂
Peso molecular:466.33

Almacenamiento:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

JI-101 Chemical Structure

No. CAS: 900573-88-8

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Actividad biológica
- Descripciòn
- IC₅₀ & Target
- In Vitro
- In Vivo
- Ensayo clínico
Chemical Information
Solvente y solubilidad
- In Vitro
- In Vivo
Protocolo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

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

IC₅₀ & Target^[1]

VEGFR2

PDGFRβ

Ver todos los productos específicos de isoformas Ephrin Receptor :

EphB
EphA

Ver todos los productos específicos de isoformas PDGFR :

Ver todos los productos específicos de isoformas VEGFR :

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.

In Vivo

JI-101excreted through bile along with its mono- and di-hydroxy metabolites. Following oral administration, JI-101 is rapidly absorbed, reaching C_max within 2?h. The t_1/2 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.

Ensayo clínico

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

No. CAS 900573-88-8
Appearance Solid
Peso molecular 466.33
Fòrmula C₂₂H₂₀BrN₅O₂
Color White to off-white
SMILES

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

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvente y solubilidad

In Vitro:

DMSO : ≥ 100 mg/mL (214.44 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

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

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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocolo

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].

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

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (275 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Gurav SD, et al. 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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.1444 mL	10.7220 mL	21.4440 mL	53.6101 mL
	5 mM	0.4289 mL	2.1444 mL	4.2888 mL	10.7220 mL
	10 mM	0.2144 mL	1.0722 mL	2.1444 mL	5.3610 mL
	15 mM	0.1430 mL	0.7148 mL	1.4296 mL	3.5740 mL
	20 mM	0.1072 mL	0.5361 mL	1.0722 mL	2.6805 mL
	25 mM	0.0858 mL	0.4289 mL	0.8578 mL	2.1444 mL
	30 mM	0.0715 mL	0.3574 mL	0.7148 mL	1.7870 mL
	40 mM	0.0536 mL	0.2681 mL	0.5361 mL	1.3403 mL
	50 mM	0.0429 mL	0.2144 mL	0.4289 mL	1.0722 mL
	60 mM	0.0357 mL	0.1787 mL	0.3574 mL	0.8935 mL
	80 mM	0.0268 mL	0.1340 mL	0.2681 mL	0.6701 mL
	100 mM	0.0214 mL	0.1072 mL	0.2144 mL	0.5361 mL

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JI-101

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Differentiation Inducing Compound Library

Reprogramming Compound Library

Anti-Cardiovascular Disease Compound Library

Orally Active Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Angiogenesis-Related Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Cytokine Inhibitors Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Fibrosis Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Ver todos los productos específicos de isoformas Ephrin Receptor

Ver todos los productos específicos de isoformas PDGFR

Ver todos los productos específicos de isoformas VEGFR

Actividad biológica

Chemical Information

Solvente y solubilidad

Protocolo

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

JI-101 Related Classifications

HY-16265 Related Classifications