2. Cell Cycle/DNA Damage Cytoskeleton Membrane Transporter/Ion Channel Apoptosis
  3. Microtubule/Tubulin P-glycoprotein Apoptosis CDK Bcl-2 Family
  4. Tubulin-IN-66

Tubulin-IN-66 is a tubulin (tubulin) and P-gp inhibitor with antiproliferative activity against cancer cells. Tubulin-IN-66 covalently binds to the Colchicine (HY-16569)-binding site at Cys239 of the β-tubulin subunit, inhibits tubulin polymerization and disrupts the microtubule network. Tubulin-IN-66 inhibits P-gp function to overcome multidrug resistance. Tubulin-IN-66 arrests the cell cycle at the G2/M phase and induces apoptosis (apoptosis). Tubulin-IN-66 inhibits colony formation and migration of cancer cells. Tubulin-IN-66 can be used in the research of tumors such as breast cancer.

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

Tubulin-IN-66

Tubulin-IN-66 Chemical Structure

CAS No. : 3110538-32-1

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-IN-66 Related Antibodies

Top Publications Citing Use of Products

View All CDK Isoform Specific Products:

View All Isoforms
CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

View All Bcl-2 Family Isoform Specific Products:

View All Isoforms
Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3 Bad

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Tubulin-IN-66 is a tubulin (tubulin) and P-gp inhibitor with antiproliferative activity against cancer cells. Tubulin-IN-66 covalently binds to the Colchicine (HY-16569)-binding site at Cys239 of the β-tubulin subunit, inhibits tubulin polymerization and disrupts the microtubule network. Tubulin-IN-66 inhibits P-gp function to overcome multidrug resistance. Tubulin-IN-66 arrests the cell cycle at the G2/M phase and induces apoptosis (apoptosis). Tubulin-IN-66 inhibits colony formation and migration of cancer cells. Tubulin-IN-66 can be used in the research of tumors such as breast cancer[1].

In Vitro

Tubulin-IN-66 (compound 10v) (48 h) potently inhibits the proliferation of HT-1080, MCF-7 and MDA-MB-231 cancer cells, with IC50 values of 0.30 μM, 0.24 μM and 0.48 μM, respectively[1].
Tubulin-IN-66 (50-200 nM; 8 days) potently inhibits colony formation of HT-1080 and MCF-7 cells in a concentration-dependent manner[1].
Tubulin-IN-66 (150-350 nM; 4-12 h) potently inhibits the migratory capacity of HT-1080 cells in a concentration-dependent manner[1].
Tubulin-IN-66 (5-30 μM; 90 min) inhibits the polymerization of purified tubulin in a concentration-dependent manner[1].
Tubulin-IN-66 (150-450 nM; 24 h) induces concentration-dependent G2/M cell cycle arrest in HT-1080 cells, accompanied by upregulated expression of Cyclin B1, CDK1 and p-H3[1].
Tubulin-IN-66 (150-450 nM; 48 h) induces early apoptosis in HT-1080 cells in a concentration-dependent manner, and its mechanism involves the upregulation of Bax expression and the downregulation of Bcl-2 expression[1].
Tubulin-IN-66 (150-450 nM; 48 h) reduces the mitochondrial membrane potential of HT-1080 cells in a concentration-dependent manner[1].
Tubulin-IN-66 (48 h) potently inhibits the proliferation of doxorubicin-resistant MCF-7/ADM cells, with an IC50 of 0.30 μM after 48 h of treatment. Its resistance index is 1.25, indicating extremely low drug resistance[1].
Tubulin-IN-66 (5-10 μM; 15 min) inhibits the function of P-gp in MCF-7/ADM cells[1].
Tubulin-IN-66 (48 h) exhibits cytotoxicity against human normal cells HUVEC and 293T, with IC50 values of 0.64 μM and 0.34 μM, respectively[1].

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

Tubulin-IN-66 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: HT-1080 fibrosarcoma cells, MCF-7 breast cancer cells
Concentration: 50, 100, 200 nM
Incubation Time: 8 days
Result: Inhibited colony formation in both cell lines in a concentration-dependent manner, with near-complete inhibition observed at the highest tested concentration.

Cell Cycle Analysis[1]

Cell Line: HT-1080 fibrosarcoma cells
Concentration: 150, 300, 450 nM
Incubation Time: 24 h
Result: Induced concentration-dependent G2/M phase cell cycle arrest, with a corresponding reduction in G0/G1 phase cell proportion.
Upregulated Cyclin B1, CDK1, and p-H3 protein expression in a concentration-dependent manner via Western blot.
In Vivo

Tubulin-IN-66 (10-50 mg/kg; i.p.; once every 2 days; for 14 consecutive days) exhibits dose-dependent in vivo antitumor efficacy in the mouse 4T1 breast cancer model[1].

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

Animal Model: BALB/c mice treated 4T1 cells (female, 6-8 weeks of age)[1]
Dosage: 10 mg/kg; 20 mg/kg; 50 mg/kg
Administration: i.p.; every other day; 14 days
Result: Showed no significant intergroup differences in mouse body weight, with no observable adverse effects.
Significantly decreased tumor volume and weight in a dose-dependent manner, with tumor growth inhibition (TGI) values of 46.76% (10 mg/kg), 53.96% (20 mg/kg), and 64.51% (50 mg/kg).
Exhibited no obvious pathological injury in major organs (heart, liver, spleen, lung, kidney) via hematoxylin and eosin (H&E) staining.
Molecular Weight

412.44

Formula

C22H24N2O6
CAS No.
SMILES

COC(C1=CC2=C(N(CCN2)C(/C=C/C3=CC(OC)=C(C(OC)=C3)OC)=O)C=C1)=O
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-IN-66 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-IN-663110538-32-1Microtubule/TubulinP-glycoproteinApoptosisCDKBcl-2 FamilyP-gpPgpMultidrug resistance protein 1MDR1ATP-binding cassette sub-family B member 1ABCB1Cluster of differentiation 243CD243Cyclin dependent kinasetubulin polymerizationHT-1080colchicine binding siteβ-Cys239breast cancerMDA-MB-231fibrosarcomamicrotubule networksMCF-7Inhibitorinhibitorinhibit

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-IN-66
Cat. No.:
HY-182753
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.