CCDC 2549599
CCDC 2549599 is an antitumor agent. CCDC 2549599 exhibits potent and highly selective antiproliferative activity against colorectal cancer (CRC) cells, with IC50 values of 0.057 μM and 0.067 μM against HT-29 and HCT 116 cells, respectively. CCDC 2549599 significantly inhibits colony formation and DNA synthesis in colorectal cancer cells, induces G0/G1 phase cell cycle arrest, downregulates Cyclin D1/CDK4 expression, and exerts its anticancer effect through dual downregulation of RRM2 and the mitochondrial translation machinery, leading to severe replication stress and an energy metabolism crisis. CCDC 2549599 can be used for research on colorectal cancer.
For research use only. We do not sell to patients.
- Formula: C28H38O6
- Molecular Weight:470.60
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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- References
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Biological Activity
Description
IC50 & Target
[1]|
Cdk4/cyclin D1 |
RRM2 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HT-29 | IC50 |
0.057 μM
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Cytotoxicity against human HT-29 colorectal cancer cells assessed by CCK-8 assay measuring absorbance at 450 nm.
Cytotoxicity against human HT-29 colorectal cancer cells assessed by CCK-8 assay measuring absorbance at 450 nm.
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42361483 |
| HCT-116 | IC50 |
0.067 μM
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Cytotoxicity against human HCT 116 colorectal cancer cells assessed by CCK-8 assay measuring absorbance at 450 nm.
Cytotoxicity against human HCT 116 colorectal cancer cells assessed by CCK-8 assay measuring absorbance at 450 nm.
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42361483 |
| NCM460 | IC50 |
> 30 μM
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Cytotoxicity against human NCM460 normal colon mucosal epithelial cells assessed by CCK-8 assay measuring absorbance at 450 nm; IC50 >30 μM.
Cytotoxicity against human NCM460 normal colon mucosal epithelial cells assessed by CCK-8 assay measuring absorbance at 450 nm; IC50 >30 μM.
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42361483 |
In Vitro
CCDC 2549599 (0.1-3 μM; 14 days) persistently inhibits the clonogenic survival of HT-29 and HCT 116 cells in a dose-dependent manner[1].
CCDC 2549599 (0.03-3 μM; 24-72 h) induces dose- and time-dependent morphological damage and loss of viability in HT-29 and HCT 116 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HT-29 and HCT 116 cells
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Concentration:0.1, 0.3, 1, 3 μM
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Incubation Time:14 days
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Result:Dose-dependently suppressed colony formation in both cell lines, with colony numbers progressively declining as concentration increased.
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Cell Line:HT-29 and HCT 116 cells
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Concentration:0.03, 0.1, 0.3, 1, 3 μM
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Incubation Time:24, 48, 72 h
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Result:Inhibited cell growth.
Calcein-AM/PI dual-stain fluorescence imaging confirmed a concentration-dependent decrease in the number of viable cells.
At a concentration of 3 μM, nearly all cells lost viability (mostly becoming PI-positive dead cells or showing disrupted morphology).
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Cell Line:HT-29 and HCT 116 cells
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Concentration:0.1, 0.3, 1, 3 μM
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Incubation Time:48 h; 2 h (EdU labeling)
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Result:Dose-dependently suppressed DNA synthesis.
At concentrations of 1 μM and 3 μM, EdU incorporation was almost completely blocked.
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Cell Line:HT-29 and HCT 116 cells
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Concentration:0.1, 0.3, 1, 3 μM
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Incubation Time:24 h
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Result:Induced significant G0/G1 phase arrest. After treatment, the proportion of cells in the G0/G1 phase increased from approximately 38% (HT-29) / 42% (HCT 116) in the control group to 70-76%, accompanied by a substantial decrease in the S-phase cell proportion.
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Cell Line:HT-29 and HCT 116 cells
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Concentration:0.03, 0.1, 0.3, 1, 3 μM
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Incubation Time:24 h
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Result:Significantly downregulated the expression of cell cycle-related proteins CDK4 and Cyclin D1, and markedly suppressed the expression level of RRM2, a key protein in DNA replication, even at concentrations as low as 0.1-0.3 μM.
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Cell Line:HT-29 and HCT 116 cells
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Concentration:0.03, 0.1, 0.3, 1, 3 μM
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Incubation Time:24 h
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Result:At 0.3 μM, RRM2 levels decreased by approximately 85% in HCT 116 cells and 74% in HT-29 cells.
- EdU Incorporation Assay (Click Chemistry-Based DNA Synthesis Measurement)
- RNA extraction experimental
- Flow cytometric DNA-content cell-cycle staining
- BrdU Incorporation Assay
- Protocol for Cell Cycle
- Soft Agar Colony Formation Assay
- Colony Formation (Clonogenic) Assay
- Cell Viability Determination by MTT Colorimetric Assay
Chemical Information
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Molecular Weight 470.60
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Formula C28H38O6
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SMILES
O=C(O[C@H]1O[C@@]2([H])[C@@]3(OO[C@](O2)(C)CC4)C4[C@H](C)CCC3[C@H]1C)/C=C/C5=CC=CC(C(C)(C)C)=C5
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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)
CCDC 2549599 Related Classifications
HY-190660 Related Classifications
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