2. Protein Tyrosine Kinase/RTK
  3. VEGFR
  4. VEGFR-3-IN-1

VEGFR-3-IN-1 is a potent and selective VEGFR3 inhibitor with an IC50 of 110.4 nM. VEGFR-3-IN-1 significantly inhibits proliferation and migration of VEGF-C-induced human dermal lymphatic endothelial cells (HDLEC), MDA-MB-231, and MDA-MB-436 cells by inactivating the VEGFR3 signaling pathway, and also effectively inhibits breast cancer growth.

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

VEGFR-3-IN-1 Chemical Structure

VEGFR-3-IN-1 Chemical Structure

CAS No. : 2756668-73-0

Size Price Stock Quantity
Free Sample (0.1 - 0.5 mg)   Apply Now  
5 mg USD 140 In-stock
10 mg USD 230 In-stock
25 mg USD 460 In-stock
50 mg USD 750 In-stock
100 mg USD 1200 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

VEGFR-3-IN-1 Related Antibodies

Top Publications Citing Use of Products

View All VEGFR Isoform Specific Products:

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

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

VEGFR-3-IN-1 is a potent and selective VEGFR3 inhibitor with an IC50 of 110.4 nM. VEGFR-3-IN-1 significantly inhibits proliferation and migration of VEGF-C-induced human dermal lymphatic endothelial cells (HDLEC), MDA-MB-231, and MDA-MB-436 cells by inactivating the VEGFR3 signaling pathway, and also effectively inhibits breast cancer growth[1].

IC50 & Target[1]

VEGFR3

110.4 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
MDA-MB-231 IC50
2.22 μM
Compound: 38k
Anticancer activity against human MDA-MB-231 cells assessed as cell viability incubated for 48 hrs by MTT assay
Anticancer activity against human MDA-MB-231 cells assessed as cell viability incubated for 48 hrs by MTT assay
[PMID: 34351741]
MDA-MB-436 IC50
3.5 μM
Compound: 38k
Anticancer activity against human MDA-MB-436 cells assessed as cell viability incubated for 48 hrs by MTT assay
Anticancer activity against human MDA-MB-436 cells assessed as cell viability incubated for 48 hrs by MTT assay
[PMID: 34351741]
In Vitro

VEGFR-3-IN-1 (compound 38k) exhibits a significantly higher antiproliferative activity on MDA-MB-231 and MDA-MB-436 cells than 10 (IC50 > 50 μM), with IC50 values of 2.22 and 3.50 μM, respectively[1].
VEGFR-3-IN-1 markedly suppresses the phosphorylation of VEGFR3 and its downstream proteins in a dose-dependent manner[1].

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

VEGFR-3-IN-1 Related Antibodies

Cell Viability Assay[1]

Cell Line: MDA-MB-231 and MDA-MB-436 cells
Concentration: 100 nM
Incubation Time: 48 hours
Result: Exerted antimigration and antiproliferative activities through targeting VEGFR3 in MDA-MB-231 and MDA-MB-436 cells.

Western Blot Analysis[1]

Cell Line: HDLEC cells
Concentration: 10-500 nM
Incubation Time:
Result: Antilymphangiogenic activities of VEGFR-3-IN-1 by suppressing the expression of VEGFR3.
In Vivo

VEGFR-3-IN-1 (50, 25 mg/kg; p.o.) reduces the tumor volume, and displays the strongest inhibitory activity in mice, with a growth inhibition rate of 61.9%[1].
VEGFR-3-IN-1 (10 mg/kg; p.o.) treatment shows the Cmax, AUC0-t , AUC0-∞ and t1/2 values of 420 ng/mL, 9219 ng h/mL, 12304 ng h/mL and 16 hours, respectively[1].

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

Animal Model: Nude mice (carrying xenografted BC)[1]
Dosage: 50 mg/kg
Administration: P.o.;once
Result: Reduced the tumor volume, and displayed the strongest inhibitory activity in mice.
Animal Model: Sprague-Dawley (SD) rats [1]
Dosage: 10 mg/kg
Administration: P.o. (Pharmacokinetic Analysis)
Result: The Cmax, AUC0-t , AUC0-∞ and t1/2 were 420 ng/mL, 9219 ng h/mL, 12304 ng h/mL and 16 hours, respectively.
Molecular Weight

616.10

Formula

C29H29ClF3N7OS
CAS No.
Appearance

Solid

Color

Off-white to yellow

SMILES

O=C(N1CCN(C2=C(C=C(C3=CC=C(N4CCN(C)CC4)C=C3)S5)C5=NC=N2)CC1)NC6=CC=C(Cl)C(C(F)(F)F)=C6
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 12.5 mg/mL (20.29 mM; ultrasonic and warming and adjust pH to 6 with HCl and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6231 mL 8.1156 mL 16.2311 mL
5 mM 0.3246 mL 1.6231 mL 3.2462 mL
View the Complete Stock Solution Preparation Table

* 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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

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: ≥ 1.25 mg/mL (2.03 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.6231 mL 8.1156 mL 16.2311 mL 40.5778 mL
5 mM 0.3246 mL 1.6231 mL 3.2462 mL 8.1156 mL
10 mM 0.1623 mL 0.8116 mL 1.6231 mL 4.0578 mL
15 mM 0.1082 mL 0.5410 mL 1.0821 mL 2.7052 mL
20 mM 0.0812 mL 0.4058 mL 0.8116 mL 2.0289 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

VEGFR-3-IN-1 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.

Keywords:

VEGFR-3-IN-12756668-73-0VEGFRVascular endothelial growth factor receptorhighly selectiveVEGF-CHDLECMDA-MB-231MDA-MB-436breast cancerInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
VEGFR-3-IN-1
Cat. No.:
HY-132305
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

English - EN (251 KB) Français - FR (251 KB) Deutsch - DE (251 KB) Norwegian - NO (251 KB) Español - ES (251 KB) Swedish - SV (251 KB)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.