A-259745
A-259745 is an orally active antimitotic agent that binds to the colchicine-binding site of tubulin. A-259745 exhibits potent in vitro cytotoxic activity against both multi-drug-resistant and non-multi-drug-resistant cancer cell lines, with ED50 values of 0.018 μM against HCT-15 and 0.028 μM against NCI-H460 cell lines. A-259745 inhibits tubulin polymerization, disrupts the dynamic equilibrium of the mitotic spindle, arrests dividing cells in metaphase, and subsequently induces apoptosis. A-259745 shows dose-dependent antitumor efficacy in murine tumor models. A-259745 can be used for the study of cancer.
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- No. CAS: 256934-83-5
- Fòrmula: C21H22N2O4
- Peso molecular:366.41
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-15 | ED50 |
0.018 μM
Compound: 22g
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Effective dose against HCT-15 cell line.
Effective dose against HCT-15 cell line.
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[PMID: 11728187] |
| HCT-15 | IC50 |
16 nM
Compound: 5b
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Antiproliferative activity against the MDR positive human colon adenocarcinoma cell line HCT-15
Antiproliferative activity against the MDR positive human colon adenocarcinoma cell line HCT-15
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[PMID: 11814821] |
| NCI-H460 | ED50 |
0.028 μM
Compound: 22g
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Effective dose against NCI-H460 cell line.
Effective dose against NCI-H460 cell line.
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[PMID: 11728187] |
| NCI-H460 | IC50 |
14 nM
Compound: 5b
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Antiproliferative activity against the human non small cell lung carcinoma cell line NCI-H460
Antiproliferative activity against the human non small cell lung carcinoma cell line NCI-H460
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[PMID: 11814821] |
Chemical Information
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No. CAS 256934-83-5
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Peso molecular 366.41
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Fòrmula C21H22N2O4
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SMILES
CN1C=CC2=C1C=CC(C3=NCC(C4=CC(OC)=C(OC)C(OC)=C4)O3)=C2
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Synonyms
A-289099
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
A-259745 Related Classifications
HY-101741 Related Classifications
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