2. Protein Tyrosine Kinase/RTK Cytoskeleton Cell Cycle/DNA Damage Immunology/Inflammation NF-κB Metabolic Enzyme/Protease Apoptosis
  3. VEGFR Microtubule/Tubulin Reactive Oxygen Species (ROS) Apoptosis
  4. Tubulin/VEGFR-2-IN-2

Tubulin/VEGFR-2-IN-2 is an orally active tubulin and VEGFR-2 inhibitor with IC50s of 3.27 and 0.09 μM, respectively. Tubulin/VEGFR-2-IN-2 exerts the antitumor effects through multifaceted pathways, including enhancing reactive oxygen species (ROS) generation, disrupting mitochondrial membrane potential, inducing apoptosis, and arresting the cell cycle. Tubulin/VEGFR-2-IN-2 demonstrates anti-angiogenic properties by significantly impairing endothelial cell migration, invasion, and tube formation in vitro. Tubulin/VEGFR-2-IN-2 suppresses angiogenesis, tumor growth, and metastasis in vivo. Tubulin/VEGFR-2-IN-2 can be used for non-small lung cancer, breast cancer, gastric cancer and lymphoma.

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

Tubulin/VEGFR-2-IN-2

Tubulin/VEGFR-2-IN-2 Chemical Structure

CAS No. : 2882998-56-1

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  

* Please select Quantity before adding items.

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

Tubulin/VEGFR-2-IN-2 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

Tubulin/VEGFR-2-IN-2 is an orally active tubulin and VEGFR-2 inhibitor with IC50s of 3.27 and 0.09 μM, respectively. Tubulin/VEGFR-2-IN-2 exerts the antitumor effects through multifaceted pathways, including enhancing reactive oxygen species (ROS) generation, disrupting mitochondrial membrane potential, inducing apoptosis, and arresting the cell cycle. Tubulin/VEGFR-2-IN-2 demonstrates anti-angiogenic properties by significantly impairing endothelial cell migration, invasion, and tube formation in vitro. Tubulin/VEGFR-2-IN-2 suppresses angiogenesis, tumor growth, and metastasis in vivo. Tubulin/VEGFR-2-IN-2 can be used for non-small lung cancer, breast cancer, gastric cancer and lymphoma[1].

IC50 & Target[1]

VEGFR2

0.09 μM (IC50)

Tubulin

3.27 nM (IC50)

In Vitro

Tubulin/VEGFR-2-IN-2 (compound 19d) (48 h) displays superior anti-proliferative effects across a panel of cancer cell lines (IC50 = 0.26, 0.19, 0.04, 0.04, 12.06 and 4.70 μM for A549, MCF-7, MGC-803, U937 cell, HEK 293 T and RAW 264.7 cells respectively) [1].
Tubulin/VEGFR-2-IN-2 (0-20 nM, 24 h) exhibits potent anti-proliferation effects in MGC-803 cells[1].
Tubulin/VEGFR-2-IN-2 (25-100 nM, 48 h) suppresses cell proliferation by interfering with the polymerization process of tubulin in MGC-803 cells[1].
Tubulin/VEGFR-2-IN-2 (25-100 nM, 48 h) reduces the Mitochondrial membrane potential, exhibits apoptosis by activating the caspase family proteins, induces considerable DNA damage and oxidative stress, causes G2/M phase cell cycle arrest and impairs the migratory and invasive ability with a dose-dependent manner in MGC-803 cells[1].
Tubulin/VEGFR-2-IN-2 (20-80 nM, 6-8 h or 48 h) inhibits angiogenesis (including impairs angiogenic structures, destroys the tubular network, decreases nodes, master junctions, segment length, total branching length, meshes, and mean density) by suppressing of the VEGFR-2- driven PI3K/AKT/MAPK pathway in human umbilical vein endothelial cell (HUVEC)[1].
Tubulin/VEGFR-2-IN-2 (20-80 nM, 48 h) inhibits endothelial cell migration and invasion in HUVEC[1].

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

Tubulin/VEGFR-2-IN-2 Related Antibodies

Cell Cycle Analysis[1]

Cell Line: MGC-803 cells
Concentration: 25, 50, 100 nM
Incubation Time: 48 h
Result: Led to a concentration-dependent increase in the proportion of cells in the G2/M phase.

Immunofluorescence[1]

Cell Line: MGC-803 cells
Concentration: 25, 50, 100 nM
Incubation Time: 48 h
Result: Transformed from the typical elongated, spindle-like configuration into a rounded form.

Apoptosis Analysis[1]

Cell Line: MGC-803 cells
Concentration: 25, 50, 100 nM
Incubation Time: 48 h
Result: Exhibited concentration-dependent apoptosis.

Western Blot Analysis[1]

Cell Line: MGC-803 cells
Concentration: 25, 50, 100 nM
Incubation Time: 48 h
Result: Led An upregulation of Cyt-C and the pro-apoptotic protein Bax, accompanied by a downregulation of the anti-apoptotic protein Bcl-2.
Increased in γH2AX expression.
Led a reduction of Cyclin B1 and phosphorylated Cdc2 (p-Cdc2) expression and a marked downregulation of the cell cycle inhibitor P21.
Reduced the phosphorylation of ERK, downregulated the mesenchymal markers Vimentin and N-cadherin, and upregulated the epithelial marker E-cadherin in a dose-dependent manner.
Led to a significant reduction in the expression of both FAK and MMP-9.

Cell Proliferation Assay[1]

Cell Line: MGC-803 cells
Concentration: 0, 1.25, 2.5, 5, 10 and 20 nM
Incubation Time: 24 h
Result: Decreased significantly the number and the size of colonies formed.

Cell Migration Assay [1]

Cell Line: MGC-803 cells
Concentration: 25, 50, 100 nM
Incubation Time: 48 h
Result: Exhibited a significant reduction.
Had an inverse correlation with the invasive capacity of MGC-803 cells.

Western Blot Analysis[1]

Cell Line: HUVEC cells
Concentration: 20, 40 and 80 nM
Incubation Time: 48 h
Result: Markedly reduced VEGFR-2 expression and attenuated the phosphorylation of PI3K, AKT, and ERK.
Parmacokinetics
Species Dose Route Cmax T1/2 Tmax AUC0-24 CL F
Rat[1] 10 mg/kg p.o. 1846 ng/mL 5.8 h 25 min 3054 μg/L·h 51.6 mL/min/kg 77 %
Rat[1] 5 mg/kg i.v. 1026 ng/mL 3.4 h 12 min 1984 ng/L.h 18.5 mL/min/kg /
In Vivo

Tubulin/VEGFR-2-IN-2 (compound 19d) (100-400 nM in 1 mL water, 18 h) can inhibits angiogenesis in Tg (flk: EGFP) zebrafish embryos[1].
Tubulin/VEGFR-2-IN-2 (100-400 nM in 1 mL water, 72 h) effectively inhibits both tumor growth and metastasis in vivo in a dose-dependent manner in fluorescently labeled MGC-803 cells induced-Tg (flk: EGFP) zebrafish larvae[1].

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

Animal Model: Tg(flk: EGFP) zebrafish embryos[1]
Dosage: 100 nM, 200 nM, and 400 nM
Administration: Maintained in 1 mL aquaculture water with different dosage for 18 h
Result: Produced a dose-responsive decline in both , intersegmental vessels (ISVs) count and vessel length.
Animal Model: Fluorescently labeled MGC-803 cells (300-500 cells) induced-Tg(flk: EGFP) zebrafish larvae[1]
Dosage: 100 nM, 200 nM, and 400 nM
Administration: Maintained in 1 mL aquaculture water with different dosage for 18 h
Result: Suppressed tumor cell migration in a dose-dependent manner.
The tumor mass was significantly decreased at the highest concentration.
Molecular Weight

366.41

Formula

C20H22N4O3
CAS No.
SMILES

NC1=CC(C2=NC(NC3=CC(OC)=C(C(OC)=C3)OC)=NC=C2)=CC=C1C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
  • 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.

Tubulin/VEGFR-2-IN-2 Related Classifications

  • 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
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:

Tubulin/VEGFR-2-IN-22882998-56-1VEGFRMicrotubule/TubulinReactive Oxygen Species (ROS)ApoptosisVascular endothelial growth factor receptorVEGFR-2tubulinROSapoptosisdual-target anti-cancerInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Tubulin/VEGFR-2-IN-2
Cat. No.:
HY-180292
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)

Request for HNMR Report

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