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.
For research use only. We do not sell to patients.
- CAS No.: 2417134-05-3
- Formula: C15H15ClN2O2
- Molecular Weight:290.74
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
IC50: 3.15 μM (tubulin polymerization)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| H22 | IC50 |
0.017 μM
Compound: 20a
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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
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[PMID: 32339853] |
| HepG2 | IC50 |
0.019 μM
Compound: 20a
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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
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[PMID: 32339853] |
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.
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Cell Line:K562 cells
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Concentration:0-1 μM
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Incubation Time:72 h
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Result:Showed anti-proliferative activity with an IC50 of 0.01 ± 0.001 μM against K562 cells.
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Cell Line:HepG2, HCT-8, MDA-MB-231 and HFL-1 cells
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Concentration:0-1 μM
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Incubation Time:72 h
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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.
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Cell Line:K562 cells
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Concentration:5 nM, 10 nM and 20 nM
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Incubation Time:48 h
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Result:9.40%, 11.54% and 15.28% of cells were arrested at G2/M phase at 5, 10 and 20 nM, respectively.
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Cell Line:K562 cells
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Concentration:5 nM, 10 nM and 20 nM
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Incubation Time:48 h
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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.
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Cell Line:HUVECs
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Concentration:5 nM, 10 nM and 20 nM
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Incubation Time:24 h
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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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Five-week-old male ICR mice, liver tumor allograft model[1]
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Dosage:15 and 30 mg/kg
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Administration:Intravenous injection, daily for 21 days
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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.
Chemical Information
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CAS No. 2417134-05-3
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Molecular Weight 290.74
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Formula C15H15ClN2O2
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SMILES
C=C(C1=CC(Cl)=NC(NC)=C1)C2=CC=C(C(O)=C2)OC
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)