Microtubule inhibitor 2
Microtubule inhibitor 2 is a potent and selective, orally active microtubule inhibitor. Microtubule inhibitor 2 triggers cell death through ferroptosis . Microtubule inhibitor 2 shows antitumor activity.
For research use only. We do not sell to patients.
- CAS No.: 3031328-45-4
- Formula: C20H23NO7
- Molecular Weight:389.40
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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
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A2780 | IC50 |
0.02 μM
Compound: 33
|
Antiproliferative activity against human A2780 cells assessed as cell viability incubated for 48 hrs by MTT assay
Antiproliferative activity against human A2780 cells assessed as cell viability incubated for 48 hrs by MTT assay
|
[PMID: 35282680] |
| A2780 | IC50 |
0.04 μM
Compound: 33
|
Antiproliferative activity against human paclitaxel-resistant A2780/TAX cells assessed as cell viability incubated for 48 hrs by MTT assay
Antiproliferative activity against human paclitaxel-resistant A2780/TAX cells assessed as cell viability incubated for 48 hrs by MTT assay
|
[PMID: 35282680] |
| A549 | IC50 |
0.01 μM
Compound: 33
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Antiproliferative activity against human A549 cells assessed as cell viability incubated for 48 hrs by MTT assay
Antiproliferative activity against human A549 cells assessed as cell viability incubated for 48 hrs by MTT assay
|
[PMID: 35282680] |
| A549 | IC50 |
0.01 μM
Compound: 33
|
Cytotoxicity against human A549 cells assessed as reduction in cell viability
Cytotoxicity against human A549 cells assessed as reduction in cell viability
|
[PMID: 35282680] |
| A549 | IC50 |
0.02 μM
Compound: 33
|
Antiproliferative activity against human adriamycin-resistant A549/ADR cells assessed as cell viability incubated for 48 hrs by MTT assay
Antiproliferative activity against human adriamycin-resistant A549/ADR cells assessed as cell viability incubated for 48 hrs by MTT assay
|
[PMID: 35282680] |
| HCT-8 | IC50 |
0.04 μM
Compound: 33
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Antiproliferative activity against human HCT-8 cells assessed as cell viability incubated for 48 hrs by MTT assay
Antiproliferative activity against human HCT-8 cells assessed as cell viability incubated for 48 hrs by MTT assay
|
[PMID: 35282680] |
| HCT-8 | IC50 |
0.07 μM
Compound: 33
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Antiproliferative activity against human vincristine-resistant HCT-8/VCR cells assessed as cell viability incubated for 48 hrs by MTT assay
Antiproliferative activity against human vincristine-resistant HCT-8/VCR cells assessed as cell viability incubated for 48 hrs by MTT assay
|
[PMID: 35282680] |
| HeLa | IC50 |
0.02 μM
Compound: 33
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Antiproliferative activity against human HeLa cells assessed as cell viability incubated for 48 hrs by MTT assay
Antiproliferative activity against human HeLa cells assessed as cell viability incubated for 48 hrs by MTT assay
|
[PMID: 35282680] |
| HUVEC | IC50 |
0.04 μM
Compound: 33
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Cytotoxicity against HUVEC cells assessed as reduction in cell viability
Cytotoxicity against HUVEC cells assessed as reduction in cell viability
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[PMID: 35282680] |
| L02 | IC50 |
1.45 μM
Compound: 33
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Cytotoxicity against human L02 cells assessed as reduction in cell viability
Cytotoxicity against human L02 cells assessed as reduction in cell viability
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[PMID: 35282680] |
| MCF-10A | IC50 |
0.54 μM
Compound: 33
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Cytotoxicity against human MCF-10A cells assessed as reduction in cell viability
Cytotoxicity against human MCF-10A cells assessed as reduction in cell viability
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[PMID: 35282680] |
| MCF7 | IC50 |
0.05 μM
Compound: 33
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Antiproliferative activity against human MCF7 cells assessed as cell viability incubated for 48 hrs by MTT assay
Antiproliferative activity against human MCF7 cells assessed as cell viability incubated for 48 hrs by MTT assay
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[PMID: 35282680] |
Microtubule inhibitor 2 (compound 33) (48 h) shows antiproliferative activity with IC50 values of 0.01, 0.02, 0.02, 0.04, 0.05 µM for A549, Hela, A2780, HCT-8, MCF-7 cells, respectively[1].
Microtubule inhibitor 2 shows selective toward normal human cells and cancer cells (IC50s of 0.01, 0.04, 1.45, 1.32,0.54 µM for A549, quiescent HUVECs, LO2, HLF, MCF-10A cells, respectively)[1].
Microtubule inhibitor 2 (48 h) shows antiproliferative activity toward drug-resistant cancer cells (IC50s of 0.02, 0.07, 0.04 for A549/ADM, HCT-8/VCR, A2780/TAX cells, respectively)[1].
Microtubule inhibitor 2 (5, 10, 20 nM; 24 h) dramatically disrupts the dynamic balance of the tubulin−microtubule system, induces the multipolarization of the mitotic spindle, and interfered with the mitosis of A549 cells[1].
Microtubule inhibitor 2 (5, 10, 20 nM, 24 h, 48 h) arrests cell cycle progression at the G2/M phase in a dose and time-dependent manner[1].
Microtubule inhibitor 2 triggers cell death through ferroptosis rather than apoptosis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549, Hela, A2780, HCT-8, MCF-7 cells
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Concentration:
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Incubation Time:48 h
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Result:Showed antiproliferative activities with IC50 values of 0.01, 0.02, 0.02, 0.04, 0.05 µM for A549, Hela, A2780, HCT-8, MCF-7 cells, respectively.
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Cell Line:A549 cells
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Concentration:5, 10, 20 nM
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Incubation Time:24 h, 48 h
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Result:Arrested cell cycle progression at the G2/M phase in a dose and time-dependent manner.
Microtubule inhibitor 2 (10 mg/kg; i.p.; every other day for 22 days) shows antitumor activity and the level of tumor growth inhibition was 78.63%[1].
Pharmacokinetic Parameters of Microtubule inhibitor 2 in Male Institute of Cancer Research (ICR) mice (18−23 g)[1].
| p.o. | i.v. | |
| dose (mg/kg) | 10 | 1 |
| T1/2 (h) | 2.12 | 0.62 |
| Tmax (h) | 0.25 | 0.08 |
| Tmax (ng/mL) | 776.31 | 871.40 |
| AUC(0-t) (h ng-1 mL) | 2432.04 | 350.19 |
| AUC(0-∞) (h ng-1 mL) | 2463.76 | 353.02 |
| MRT (h) | 2.57 | 0.68 |
| CL (mL h-1 kg-1) | - | 2855.67 |
| F % | 69.45 | - |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Institute of Cancer Research (ICR) mice (18−23 g) [1]
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Dosage:10 mg/kg
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Administration:
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Result:Displayed excellent oral bioavailability (F% = 69.45).
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Animal Model:Male BALB/c nude mice (5 weeks old, 18−20 g) (A549 xenograft models) [1]
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Dosage:10 mg/kg
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Administration:i.p.; every other day, 22 days
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Result:Showed antitumor activity and the level of tumor growth inhibition was 78.63%.
Chemical Information
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CAS No. 3031328-45-4
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Molecular Weight 389.40
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Formula C20H23NO7
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SMILES
C=C(C1=CC=C(C(O)=C1NC(CO)=O)OC)C2=CC(OC)=C(C(OC)=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)
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