Tubulin polymerization-IN-6
Tubulin polymerization-IN-6 (compound 5f) is a potent tubulin polymerization inhibitor, with an IC50 of 1.09 μM. Tubulin polymerization-IN-6 inhibits cell migration and tube formation and contributes to the anti-angiogenesis. Tubulin polymerization-IN-6 can greatly inhibit tumor growth on HT29 xenograft Balb/c nude mice.
For research use only. We do not sell to patients.
- CAS No.: 2768613-52-9
- Formula: C19H21NO7
- Molecular Weight:375.37
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
IC50: 1.09 μM (Tubulin polymerization)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
0.24 μM
Compound: 5f
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Cytotoxicity against human A549 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
Cytotoxicity against human A549 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
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[PMID: 35447432] |
| HeLa | IC50 |
0.035 μM
Compound: 5f
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Cytotoxicity against human HeLa cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
Cytotoxicity against human HeLa cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
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[PMID: 35447432] |
| HT-29 | IC50 |
0.023 μM
Compound: 5f
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Cytotoxicity against human HT-29 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
Cytotoxicity against human HT-29 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
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[PMID: 35447432] |
| MCF7 | IC50 |
0.14 μM
Compound: 5f
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Cytotoxicity against human MCF7 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
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[PMID: 35447432] |
| MDA-MB-231 | IC50 |
0.1 μM
Compound: 5f
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Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability measured after 24 hrs by MTT assay
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[PMID: 35447432] |
Tubulin polymerization-IN-6 (compound 5f) (0-20 μM, 24 h) shows a broad spectrum of anti-proliferation activity against cancer cell lines[1].
Tubulin polymerization-IN-6 (0-100 nM, 24 h) inhibits tumor cells colony formation, up-regulates the expression of Ac-α-tubulin and DeY-α-tubulin [1].
Tubulin polymerization-IN-6 (0-5 μM, 1 h) competes with colchicine and directly binds to the colchicine binding site, thus inhibit tubulin polymerization[1].
Tubulin polymerization-IN-6 (0-250 nM, 24 h) possesses a favorable anti-migration activity against cancer cells[1].
Tubulin polymerization-IN-6 (0-50 nM, 24 h) has the ability to inhibit the angiogenesis of HUVEC cells[1].
Tubulin polymerization-IN-6 (0-100 nM, 24 h) induces cell cycle arrest by regulating associated proteins, induces apoptosis by regulating associated proteins and down-regulating mitochondrial membrane potential, and dose-dependently promotes the production of ROS in HT29 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HT29, MCF-7, HeLa, MDA-MB-231, A549[1]
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Concentration:0-20 μM
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Incubation Time:24 h
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Result:Had a broad spectrum of anti-proliferation activity against cancer cell lines (MCF-7, MDA-MB-231, A549, Hela, and HT29), with IC50 values of 0.14 ± 0.03, 0.10 ± 0.00, 0.24 ± 0.03, 0.035 ± 0.002, and 0.023 ± 0.001 μM, respectively; and showed moderate anti-proliferative activity against drug resistant cancer cells (MCF-7/TxR and A549/TxR), with IC50 values of 0.18 ± 0.02 and 0.31 ± 0.08 μM, and DRI (drug-resistant index) of 1.3 and 1.2, respectively.
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Cell Line:HT29 cells[1]
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Concentration:0, 25, 50, and 100 nM
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Incubation Time:24 h
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Result:Up-regulated the expression of Ac-α-tubulin (acetyl-α-tubulin) and DeY-α-tubulin (detyrosinated-α-tubulin); regulated the expressions of the proteins involved in cell cycle such as cdc25c, cdk7, cyclin B1, and cdc2; down-regulated the level of Bim and up-regulated the levels of Bcl-2, p-Bcl-2, and Bax, decreased the expression of p-Histone H3(Ser10) and increased the expression of cleaved-Caspase-9, cleaved-Caspase-3, PARP, and cleaved-PARP.
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Cell Line:HT29 cells[1]
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Concentration:0, 25, 50, and 100 nM
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Incubation Time:6 h
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Result:Dose-dependently depolymerized the tubulin polymers into oligomers, and caused the microtubule network to collapse in HT29 cells.
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Cell Line:HT29 cells[1]
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Concentration:0, 12.5, 25, 50, and 100 nM
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Incubation Time:24 h
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Result:Induced a dose dependent G2/M phase arrest, increased the proportion of G2/M phase cells from 20.9% to 87.5% at 100 nM.
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Cell Line:HT29 cells[1]
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Concentration:0, 25, 50, and 100 nM
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Incubation Time:24 h
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Result:Induced apoptosis, increased the percentages of total apoptosis cells, down-regulated mitochondrial membrane potential.
Tubulin polymerization-IN-6 (SD rats, 10 mg/kg, IV, once) shows the better pharmacokinetic properties[1]. Pharmacokinetic Parameters of Tubulin polymerization-IN-6 in SD rats[1].
| Parameters | 5f |
| t1/2 (h) | 1.73 |
| AUC (μg/L·h) | 5.67 |
| MRT (h) | 1.92 |
| CL (L/h/kg) | 1.76 |
| Tmax (h) | 0.14 |
| Cmax (ng/mL) | 6.88 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Immunodeficient Balb/c nude mice (HT29 xenograft, 5-week-old, 36 mice, six groups)[1]
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Dosage:0, 5, 7.5, 10 mg/kg
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Administration:IP, once every two days, for three weeks
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Result:Dose-dependently inhibited the tumor growth, inhibits the tumor weight growth by 75.5% at 10 mg/kg.
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Animal Model:SD rats (5-week-old)[1]
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Dosage:10 mg/kg
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Administration:IV, once (Pharmacokinetic Analysis)
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Result:Showed the better pharmacokinetic properties, exhibited an eight-fold half-life and a two-fold AUC improvement.
Chemical Information
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CAS No. 2768613-52-9
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Molecular Weight 375.37
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Formula C19H21NO7
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SMILES
COC(C1=CC2=C(OCCO2)C=C1NC3=CC(OC)=C(C(OC)=C3)OC)=O
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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)
Tubulin polymerization-IN-6 Related Classifications
HY-146505 Related Classifications
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