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

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.

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Tubulin polymerization-IN-14 Chemical Structure

Tubulin polymerization-IN-14 Chemical Structure

CAS No. : 2417134-05-3

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Tubulin polymerization-IN-14 Related Antibodies

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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]
Cellular Effect
Cell Line Type Value Description References
H22 IC50
0.017 μM
Compound: 20a
Antiproliferative activity against mouse H22 cells assessed as inhibition of cell growth by MTT assay
Antiproliferative activity against mouse H22 cells assessed as inhibition of cell growth by MTT assay
[PMID: 32339853]
HepG2 IC50
0.019 μM
Compound: 20a
Antiproliferative against human HepG2 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
Antiproliferative against human HepG2 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
[PMID: 32339853]
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].

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

Tubulin polymerization-IN-14 Related Antibodies

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].

MedChemExpress (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

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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Tubulin polymerization-IN-14 Related Classifications

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Help & FAQs
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    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 polymerization-IN-142417134-05-3Microtubule/TubulinApoptosisK562anti-vascularanticancertubulin polymerizationInhibitorinhibitorinhibit

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