2. Cytoskeleton Cell Cycle/DNA Damage Apoptosis
  3. Microtubule/Tubulin Apoptosis
  4. 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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A-259745

A-259745 Chemical Structure

CAS No. : 256934-83-5

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A-259745 Related Antibodies

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Description

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[1].

Cellular Effect
Cell Line Type Value Description References
HCT-15 ED50
0.018 μM
Compound: 22g
Effective dose against HCT-15 cell line.
Effective dose against HCT-15 cell line.
[PMID: 11728187]
HCT-15 IC50
16 nM
Compound: 5b
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
[PMID: 11814821]
NCI-H460 ED50
0.028 μM
Compound: 22g
Effective dose against NCI-H460 cell line.
Effective dose against NCI-H460 cell line.
[PMID: 11728187]
NCI-H460 IC50
14 nM
Compound: 5b
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
[PMID: 11814821]
Molecular Weight

366.41

Formula

C21H22N2O4
CAS No.
SMILES

CN1C=CC2=C1C=CC(C3=NCC(C4=CC(OC)=C(OC)C(OC)=C4)O3)=C2
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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A-259745 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

A-259745256934-83-5A-289099A259745A 259745A289099A 289099Microtubule/TubulinApoptosisAntimitoticHCT-15NCI-H460cancertubulinInhibitorinhibitorinhibit

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