Antiproliferative agent-52
Antiproliferative agent-52 is a tubulin inhibitor with a porcine tubulin KD of 29.65 μM. Antiproliferative agent-52 binds to the colchicine-binding site at the α-tubulin and β-tubulin interface and inhibits tubulin polymerization. Antiproliferative agent-52 exhibits antiproliferative activity against tumor cells. Antiproliferative agent-52 serves as a lead compound for development of thienopyrimidine and heterocyclic fused pyrimidines with antiproliferative activity. Antiproliferative agent-52 can be used for the research of ovarian cancer, non-small cell lung cancer.
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- CAS. Nr.: 2913194-20-2
- Formel: C14H12ClN3OS
- Molecular Weight:305.78
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biologische Aktivität
Beschreibung
Cellular Effect
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A2780 | IC50 |
7.26 nM
Compound: 4a
|
Antiproliferative activity against human A2780 cells incubated for 48 hrs by CCK8 assay
Antiproliferative activity against human A2780 cells incubated for 48 hrs by CCK8 assay
|
[PMID: 38972078] |
| A549 | IC50 |
8.63 nM
Compound: 4a
|
Antiproliferative activity against human A549 cells incubated for 48 hrs by CCK8 assay
Antiproliferative activity against human A549 cells incubated for 48 hrs by CCK8 assay
|
[PMID: 38972078] |
| HCC827 | IC50 |
8.55 nM
Compound: 4a
|
Antiproliferative activity against human HCC827 cells incubated for 48 hrs by CCK8 assay
Antiproliferative activity against human HCC827 cells incubated for 48 hrs by CCK8 assay
|
[PMID: 38972078] |
| SK-OV-3 | IC50 |
5.83 nM
Compound: 4a
|
Antiproliferative activity against human SK-OV-3 cells incubated for 48 hrs by CCK8 assay
Antiproliferative activity against human SK-OV-3 cells incubated for 48 hrs by CCK8 assay
|
[PMID: 38972078] |
In Vitro
Antiproliferative agent-52 (compound 4a) (48 h) potently inhibits the proliferation of A549, A2780, SKOV3, and HCC827 human tumor cells with IC50 values ranging from 5.83 to 8.63 nM[1].
Antiproliferative agent-52 (2-14 h) binds to the colchicine binding site of tubulin within the T2R-TTL complex via hydrophobic interactions, with no hydrogen bonds formed with tubulin residues[1].
Antiproliferative agent-52 binds directly to purified tubulin with a KD of 29.65 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 2913194-20-2
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Molecular Weight 305.78
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Formel C14H12ClN3OS
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SMILES
COC1=CC=C(N(C2=NC(Cl)=NC3=C2SC=C3)C)C=C1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)