1. Cell Cycle/DNA Damage
    Cytoskeleton
    Apoptosis
  2. Microtubule/Tubulin
    Apoptosis
  3. Tubulin polymerization-IN-14

Tubulin polymerization-IN-14 

Cat. No.: HY-146211
Handling Instructions

Tubulin polymerization-IN-14 (Compound 20a) is a tubulin polymerization inhibitor with an IC50 of 3.15 μM. Tubulin polymerization-IN-14 shows potent anti-vascular and anticancer activities, induces cancer cell apoptosis.

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

Tubulin polymerization-IN-14 Chemical Structure

Tubulin polymerization-IN-14 Chemical Structure

CAS No. : 2417134-05-3

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Description

Tubulin polymerization-IN-14 (Compound 20a) is a tubulin polymerization inhibitor with an IC50 of 3.15 μM. Tubulin polymerization-IN-14 shows potent anti-vascular and anticancer activities, induces cancer cell apoptosis[1].

IC50 & Target

IC50: 3.15 μM (tubulin polymerization)[1]

In Vitro

Tubulin polymerization-IN-14 (Compound 20a) binds to the colchicine binding site on tubulin[1].
Tubulin polymerization-IN-14 (0-1 μM; 72 h) inhibits cancer cell growth[1].
Tubulin polymerization-IN-14 (5-20 nM; 48 h) arrests K562 cell cycle at G2/M phase, significantly induces cell apoptosis in K562 cells in a concentration-dependent manner, and induces mitochondrial membrane potential (MMP) collapse and mitochondrial dysfunction in K562 cells[1].
Tubulin polymerization-IN-14 (5-20 nM; 24 h) significantly decreases wound closure and capillary-like tubules formation in a concentration-dependent manner in HUVECs[1].

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

Cell Proliferation Assay[1]

Cell Line: K562 cells
Concentration: 0-1 μM
Incubation Time: 72 h
Result: Showed anti-proliferative activity with an IC50 of 0.01 ± 0.001 μM against K562 cells.

Cell Cytotoxicity Assay[1]

Cell Line: HepG2, HCT-8, MDA-MB-231 and HFL-1 cells
Concentration: 0-1 μM
Incubation Time: 72 h
Result: Showed cytotoxic activities with IC50s of 0.019 ± 0.002, 0.021 ± 0.003, 0.02 ± 0.001 and 0.118 ± 0.007 μM against HepG2, HCT-8, MDA-MB-231 and HFL-1 cells, respectively.

Cell Cycle Analysis[1]

Cell Line: K562 cells
Concentration: 5 nM, 10 nM and 20 nM
Incubation Time: 48 h
Result: 9.40%, 11.54% and 15.28% of cells were arrested at G2/M phase at 5, 10 and 20 nM, respectively.

Apoptosis Analysis[1]

Cell Line: K562 cells
Concentration: 5 nM, 10 nM and 20 nM
Incubation Time: 48 h
Result: Compared to the percentage of apoptosis cells in control group (3.25%), the total percentage of the early (Annexin-Vþ/PI) and late (Annexin-Vþ/PIþ) apoptosis cells were 10.46%, 48.55% and 62.26% after being treated at 5, 10, and 20 nM for 48 h, respectively.

Cell Migration Assay [1]

Cell Line: HUVECs
Concentration: 5 nM, 10 nM and 20 nM
Incubation Time: 24 h
Result: After exposed to compound at 5, 10, and 20 nM for 24 h, cells migrated into 67.6%, 55.3% and 49.2% of the wound area, respectively.
In Vivo

Tubulin polymerization-IN-14 (Compound 20a) (15 and 30 mg/kg; i.v.; daily for 21 days) displays obvious and dose-dependent antitumor effect with no significant toxicity in the liver tumor allograft mouse model[1].

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

Animal Model: Five-week-old male ICR mice, liver tumor allograft model[1]
Dosage: 15 and 30 mg/kg
Administration: Intravenous injection, daily for 21 days
Result: The decrease in tumor weight reached 68.7% at doses of 30 mg/kg per day at 21 days after initiation of treatment as compared to vehicle without obvious loss of body weight.
Molecular Weight

290.74

Formula

C15H15ClN2O2

CAS No.
SMILES

C=C(C1=CC(Cl)=NC(NC)=C1)C2=CC=C(C(O)=C2)OC

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
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Tubulin polymerization-IN-14
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