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.

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VEGFR-3-IN-1 Chemical Structure

VEGFR-3-IN-1 Chemical Structure

CAS No. : 2756668-73-0

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Based on 1 publication(s) in Google Scholar

VEGFR-3-IN-1 Related Antibodies

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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)

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.

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
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
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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

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