Tubulin polymerization-IN-4
Tubulin polymerization-IN-4 is a potent tubulin polymerization inhibitor with IC50 value of 4.6 μM. Tubulin polymerization-IN-4 can disrupt tubulin polymerization and vasculature, arrest the cell cycle at the G2/M phase, induce apoptosis, and suppress clonogenesis and migration in HeLa cells. Tubulin polymerization-IN-4 can be used for researching cervical cancer.
For research use only. We do not sell to patients.
- CAS No.: 2835559-00-5
- Formula: C21H21ClN2O4
- Molecular Weight:400.86
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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: 4.6 μM (tubulin)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | IC50 |
0.09 μM
Compound: 9j
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Antiproliferation activity against human HeLa cells assessed as reduction in cell growth measured after 48 to 72 hrs by CCK-8 assay
Antiproliferation activity against human HeLa cells assessed as reduction in cell growth measured after 48 to 72 hrs by CCK-8 assay
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[PMID: 35339837] |
| HeLa | IC50 |
0.09 μM
Compound: 9j
|
Antiproliferative activity against human HeLa cells assessed as reduction in cell growth measured after 48 to 72 hrs by CCK-8 assay
Antiproliferative activity against human HeLa cells assessed as reduction in cell growth measured after 48 to 72 hrs by CCK-8 assay
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[PMID: 35339837] |
| HK-2 | IC50 |
188 μM
Compound: 9j
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Cytotoxicity against HK-2 cells assessed as reduction in cell growth measured after 24 hrs by microplate reader analysis
Cytotoxicity against HK-2 cells assessed as reduction in cell growth measured after 24 hrs by microplate reader analysis
|
[PMID: 35339837] |
| SiHa | IC50 |
0.15 μM
Compound: 9j
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Antiproliferation activity against human SiHa cells assessed as reduction in cell growth measured after 48 to 72 hrs by CCK-8 assay
Antiproliferation activity against human SiHa cells assessed as reduction in cell growth measured after 48 to 72 hrs by CCK-8 assay
|
[PMID: 35339837] |
| SiHa | IC50 |
0.15 μM
Compound: 9j
|
Antiproliferative activity against human SiHa cells assessed as reduction in cell growth measured after 48 to 72 hrs by CCK-8 assay
Antiproliferative activity against human SiHa cells assessed as reduction in cell growth measured after 48 to 72 hrs by CCK-8 assay
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[PMID: 35339837] |
Tubulin polymerization-IN-4 (compound 9j) (0-1 μM; 48 hours) exhibits sub-micromolar inhibitory activities against HeLa, SiHa and MS751[1].
Tubulin polymerization-IN-4 (3, 6 and 12.5 μM; 0-20 min) inhibits tubulin polymerization in a concentration-dependent manner with the inhibition percentages of 39%, 54%, and 77% at 3, 6 and 12.5 μM[1].
Tubulin polymerization-IN-4 (1-100 μM; 2 hours) inhibits the formation of EBI-β-tubulin adduct in a concentration-dependent manner[1].
Tubulin polymerization-IN-4 (0.2 μM; 1 and 2 hours) disrupts the HUVEC-formed vascular tube[1].
Tubulin polymerization-IN-4 (0.1-0.4 μM; 24 hours) increases cell distribution to the G2/M phase in a concentration-dependent manner[1].
Tubulin polymerization-IN-4 (0.1-0.4 μM; 24 hours) induces apoptosis of HeLa cells[1].
Tubulin polymerization-IN-4 (20, 50, 100 nM; 14 days) reduces new colony formation and suppresses HeLa cell growth for 14 days in a dose-dependent manner[1].
Tubulin polymerization-IN-4 (0.1, 0.2 and 0.4 μM; 24 hours) effectively inhibits the migration of HeLa cells in a concentration-dependent manner[1].
Tubulin polymerization-IN-4 (0-200 μM; 24 hours) exhibits good renal safety profile, with IC50 of 188 ± 16 μM in HK-2 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HeLa, SiHa and MS751[1]
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Concentration:0-1 μM
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Incubation Time:48 hours
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Result:Exhibited sub-micromolar inhibitory activities against HeLa, SiHa and MS751 with IC50s of 0.09 ± 0.02 μM, 0.15 ± 0.01 μM, 0.11 ± 0.03 μM.
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Cell Line:HeLa cells[1]
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Concentration:0.1, 0.2 and 0.4 μM
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Incubation Time:24 hours
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Result:Increased cell distribution to the G2/M phase in a concentration-dependent way, arresting 24.7%, 47.6% and 71.7% of the cells in this phase at 0.1, 0.2 and 0.4 μM, respectively.
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Cell Line:HeLa cells[1]
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Concentration:0.1, 0.2 and 0.4 μM
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Incubation Time:24 hours
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Result:Induced 35.9%, 66.4% and 84.4% of cell population undergoing apoptosis at 0.1 μM, 0.2 μM, 0.4 μM, respectively.
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Cell Line:HK-2 cells[1]
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Concentration:0-200 μM
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Incubation Time:24 hours
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Result:Exhibited good renal safety profile, with IC50 of 188 ± 16 μM in HK-2 cells.
Tubulin polymerization-IN-4 (30 and 60 mg/kg; IP; daily for 21 days) inhibits the tumor growth, with TGI of 35% and 58% at dosing 30 and 60 mg/kg[1].
Tubulin polymerization-IN-4 (30 mg/kg; IP; single) presents the modest pharmacokinetic properties[1].
Pharmacokinetic Parameters of Tubulin polymerization-IN-4 in ICR mice[1].
| IP (30 mg/kg) | |
| T1/2 (h) | 1.56 ± 0.28 |
| Tmax (h) | 0.25 |
| Cmax (μg/L) | 6215 ± 308 |
| AUC0-t (μg/L·h) | 5609 ± 347 |
| AUC0-∞ (μg/L·h) | 5940 ± 347 |
| VZ/F (L/kg) | 11.35 ± 1.29 |
| CLZ/F (L/h/kg) | 5.05 ± 0.91 |
| MRT (h) | 1.77 ± 0.43 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2835559-00-5
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Molecular Weight 400.86
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Formula C21H21ClN2O4
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SMILES
CCOC1=CC=C(C=C1Cl)C2=C(N=CN=C2)C3=CC(OC)=C(C(OC)=C3)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)
Tubulin polymerization-IN-4 Related Classifications
HY-144786 Related Classifications
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