ASO-4625
ASO-4625 is a 20-nucleotide gapmer antisense oligonucleotide with a full phosphorothioate backbone and 2'-O-(2-methoxy) ethyl ribose modifications, which targets BCL2 mRNA and BCL2L1 mRNA. ASO-4625 downregulates Bcl-2 expression via an RNase H-dependent antisense mechanism with 100% complementarity, and downregulates Bcl-xL expression via the same mechanism with three mismatches. ASO-4625 induces Apoptosis and acts as a chemosensitizer. ASO-4625 does not significantly modulate the expression of Bcl-W, survivin, Akt, or p53 mRNA. ASO-4625 can be used in studies of breast cancer and non-small cell lung cancer.
For research use only. We do not sell to patients.
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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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Biological Activity
Description
IC50 & Target
[1]|
BCL2 |
Bcl-xL |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MDA-MB-231 | IC50 |
109 nM
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Downregulation of Bcl-2 mRNA in human MDA-MB-231 breast cancer cells measured by real-time quantitative PCR assay using the comparative CT method relative to rRNA with untreated cells as 100% expression reference.
Downregulation of Bcl-2 mRNA in human MDA-MB-231 breast cancer cells measured by real-time quantitative PCR assay using the comparative CT method relative to rRNA with untreated cells as 100% expression reference.
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15625915 |
| MDA-MB-231 | IC50 |
253 nM
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Downregulation of Bcl-xL mRNA in human MDA-MB-231 breast cancer cells measured by real-time quantitative PCR assay using the comparative CT method relative to rRNA with untreated cells as 100% expression reference.
Downregulation of Bcl-xL mRNA in human MDA-MB-231 breast cancer cells measured by real-time quantitative PCR assay using the comparative CT method relative to rRNA with untreated cells as 100% expression reference.
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15625915 |
| NCI-H125 | IC50 |
72 nM
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Downregulation of Bcl-2 mRNA in human NCI-H125 non-small cell lung cancer cells measured by real-time quantitative PCR assay using the comparative CT method relative to rRNA with untreated cells as 100% expression reference.
Downregulation of Bcl-2 mRNA in human NCI-H125 non-small cell lung cancer cells measured by real-time quantitative PCR assay using the comparative CT method relative to rRNA with untreated cells as 100% expression reference.
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15625915 |
| NCI-H125 | IC50 |
>300 nM
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Downregulation of Bcl-xL mRNA in human NCI-H125 non-small cell lung cancer cells measured by real-time quantitative PCR assay using the comparative CT method relative to rRNA with untreated cells as 100% expression reference.
Downregulation of Bcl-xL mRNA in human NCI-H125 non-small cell lung cancer cells measured by real-time quantitative PCR assay using the comparative CT method relative to rRNA with untreated cells as 100% expression reference.
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15625915 |
In Vitro
ASO-4625 (2-42 h) downregulates fully matched BCL2 mRNA more potently than mismatched BCL2L1 (Bcl-xL) mRNA in both MDA-MB-231 breast cancer and H125 lung cancer cells, with no significant off-target effects on Bcl-W, survivin, Akt, or p53 expression in MDA-MB-231 cells[1].
ASO-4625 (150-300 nM; 6-hour oligonucleotide incubation, followed by 42-hour further incubation after medium renewal; total 48 hours) reduces both Bcl-2 and Bcl-xL protein levels in MDA-MB-231 and H125 cells, with stronger downregulation of the fully complementary Bcl-2 target relative to the mismatched Bcl-xL target[1].
ASO-4625 (50-100 nM; 72 h) reduces viability of MDA-MB-231 breast cancer and H125 lung cancer cells and enhances the cytotoxic effect of multiple anticancer agents in both cell lines[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-231 breast cancer cells, NCI-H125 (H125) non-small cell lung cancer cells
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Concentration:Multiple concentrations (dose-response IC50 determination)
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Incubation Time:2 hours (initial time point); up to 42 hours (time-course analysis)
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Result:Showed downregulation of Bcl-2 mRNA with an IC50 of 109 nM and Bcl-xL mRNA with an IC50 of 253 nM in MDA-MB-231 cells.
Showed downregulation of Bcl-2 mRNA with an IC50 of 72 nM, and the IC50 for Bcl-xL mRNA downregulation was greater than 300 nM in H125 cells.
Showed detectable Bcl-xL mRNA downregulation as early as 2 hours after administration, with gradual increase over time in MDA-MB-231 cells.
Did not significantly modulate the expression of Bcl-W, survivin, Akt, or p53 mRNA in MDA-MB-231 cells.
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Cell Line:MDA-MB-231 breast cancer cells, H125 non-small cell lung cancer cells
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Concentration:150, 300 nM
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Incubation Time:6-hour oligonucleotide incubation, followed by 42-hour further incubation after medium renewal; total 48 hours
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Result:Caused visible downregulation of both Bcl-2 and Bcl-xL protein levels in MDA-MB-231 cells.
Exhibited suboptimal antisense effect on Bcl-xL protein at 150 nM, and more robust downregulation of both proteins at 300 nM in MDA-MB-231 cells.
Resulted in downregulation of both Bcl-2 and Bcl-xL protein in H125 cells, with less pronounced effect on Bcl-xL than on Bcl-2.
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Cell Line:MDA-MB-231 breast cancer cells, H125 non-small cell lung cancer cells
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Concentration:50-100 nM (single-agent and combination chemosensitization experiments)
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Incubation Time:6-hour oligonucleotide incubation, with further incubation up to 72 hours total after oligonucleotide addition
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Result:Decreased the viability of both MDA-MB-231 and H125 cells in a concentration-dependent manner.
Did not reduce cell viability below 50% as a single agent at 50-100 nM.
Augmented the anticancer agent-induced decrease in cell viability compared with the anticancer agents alone when combined with doxorubicin or paclitaxel in MDA-MB-231 cells, and with cisplatin, paclitaxel, or gemcitabine in H125 cells.
Chemical Information
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SMILES
[ASO-4625]
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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)
ASO-4625 Related Classifications
HY-188136 Related Classifications
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