Shopping Cart
Remove All
Your shopping cart is currently empty
VEGFR2-IN-84
Copy Product Info
🥰Excellent
Synonyms:
Catalog No. T219017 Copy Product Info
🥰Excellent
VEGFR2-IN-84 is an orally active, multi-target tyrosine kinase inhibitor with a naphthalene-based structure. It inhibits VEGFR2 with sub-nanomolar affinity and targets kinases such as Kit, FGFR, PDGFR, and Ret. VEGFR2-IN-84 competitively binds to the ATP binding pocket, blocking the phosphorylation of VEGFR2 and its downstream AKT/ERK signaling pathways. This significantly inhibits endothelial cell proliferation, migration, and tumor angiogenesis. It exhibits broad-spectrum antiproliferative activity against various solid tumors including liver, lung, and kidney cancers, with minimal cytotoxicity to normal cells, outperforming Lenvatinib. VEGFR2-IN-84 has favorable pharmacokinetic properties and high safety (LD50>2000 mg/kg), making it suitable for research on various malignant tumors.
VEGFR2-IN-84
Cas No. 861877-12-5
| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | 10-14 weeks | 10-14 weeks | |
| 50 mg | Inquiry | 10-14 weeks | 10-14 weeks |
For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)
Add to Quotation
For research use only—not for human use. No sales to individuals. Use as intended only.
Resource Download
Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | VEGFR2-IN-84 is an orally active, multi-target tyrosine kinase inhibitor with a naphthalene-based structure. It inhibits VEGFR2 with sub-nanomolar affinity and targets kinases such as Kit, FGFR, PDGFR, and Ret. VEGFR2-IN-84 competitively binds to the ATP binding pocket, blocking the phosphorylation of VEGFR2 and its downstream AKT/ERK signaling pathways. This significantly inhibits endothelial cell proliferation, migration, and tumor angiogenesis. It exhibits broad-spectrum antiproliferative activity against various solid tumors including liver, lung, and kidney cancers, with minimal cytotoxicity to normal cells, outperforming Lenvatinib. VEGFR2-IN-84 has favorable pharmacokinetic properties and high safety (LD50>2000 mg/kg), making it suitable for research on various malignant tumors. |
| Targets & IC50 | VEGFR2:0.303 nM (EC50) |
| In vitro | VEGFR2-IN-84 (E20) (4.92 nM; 96 h) significantly inhibits VEGF-induced proliferation of HUVEC cells with an activity approximately 10 times greater than Lenvatinib. At concentrations of 10-1000 nM over 48 hours, VEGFR2-IN-84 dose-dependently suppresses phosphorylation of VEGFR2 and its downstream targets AKT and ERK in HUVEC, A549, and HepG2 cells, demonstrating superior efficacy compared to Lenvatinib. Furthermore, VEGFR2-IN-84 exhibits weaker inhibitory activity on normal cells such as LO2, HEK293T, and BEAS-2B at 8.53-14.1 μM over 72 hours, indicating good selectivity toward tumor cells. |
| In vivo | VEGFR2-IN-84 (E20) administered at 50 mg/kg via oral gavage once daily for 21 days significantly inhibits tumor growth in male BALB/c nude mice with HepG2 liver cancer xenografts, outperforming an equivalent dose of Lenvatinib, with no significant body weight reduction observed. In male BALB/c nude mice xenograft models of A549 lung cancer, 786-O renal cell carcinoma, and 8305C thyroid cancer, VEGFR2-IN-84 administered orally at dosages of 30-60 mg/kg once daily for 20-30 days exhibits dose-dependent tumor growth inhibition, surpassing the efficacy of Lenvatinib at equivalent doses. In healthy ICR mice, VEGFR2-IN-84 administered at 2 mg/kg via tail vein injection demonstrates a moderate elimination half-life (T 1/2 = 5.05 h) and a plasma exposure level (AUC 0-∞ = 1970 ng・h/mL). |
| Molecular Weight | 470.50 |
| Formula | C25H18N4O4S |
| Cas No. | 861877-12-5 |
| Smiles | O=C(N)C1=CC=2C(=NC=CC2OC3=CC=C4C(C=CC=C4C(=O)NC5=NC=CS5)=C3)C=C1OC |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
Calculator
In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 µL Tween 80 and mix well until fully clarified.
3) Add 450 µL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
Dose Conversion
You can also refer to dose conversion for different animals. More Dose Conversion
Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
Preview
Related Tags: VEGFR2-IN-84 in vivo | VEGFR2-IN-84 in vitro | VEGFR2-IN-84 formula | VEGFR2-IN-84 molecular weight
Generate Quote
Catalog No.: Cas No.:
Add
| Size | Quantity | Unit Price | Amount | Operation |
|---|
Generate Quote
- TOP
Feedback
Hello! How can I help you today? 
Copyright © 2015-2026 TargetMol Chemicals Inc. All Rights Reserved.