ASO-5005
ASO-5005 is a 20-mer Gapmer antisense oligonucleotide modified with locked nucleic acids (LNA), featuring a full phosphorothioate backbone, which targets BCL2 mRNA and BCL2L1 mRNA. ASO-5005 downregulates Bcl-2 expression via an RNase H-dependent mechanism, with its sequence fully complementary to BCL2 mRNA; it simultaneously downregulates Bcl-xL expression via an RNase H-dependent mechanism, with three mismatches between its sequence and BCL2L1 mRNA, while LNA modification enhances its activity against this mismatched target. ASO-5005 induces Apoptosis by activating Caspase-3 and cleaving ICAD. ASO-5005 does not significantly regulate the expression of Bcl-W, Survivin, Akt, or p53 in tumor cells. ASO-5005 can be used for research on 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.
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 |
65 nM
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Downregulation of Bcl-2 mRNA in human MDA-MB-231 breast cancer cells quantified by real-time PCR using the comparative CT method relative to rRNA from three independent experiments performed in quadruplicate.
Downregulation of Bcl-2 mRNA in human MDA-MB-231 breast cancer cells quantified by real-time PCR using the comparative CT method relative to rRNA from three independent experiments performed in quadruplicate.
|
15625915 |
| MDA-MB-231 | IC50 |
97 nM
|
Downregulation of Bcl-xL mRNA in human MDA-MB-231 breast cancer cells quantified by real-time PCR using the comparative CT method relative to rRNA from three independent experiments performed in quadruplicate.
Downregulation of Bcl-xL mRNA in human MDA-MB-231 breast cancer cells quantified by real-time PCR using the comparative CT method relative to rRNA from three independent experiments performed in quadruplicate.
|
15625915 |
| NCI-H125 | IC50 |
71 nM
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Downregulation of Bcl-2 mRNA in human NCI-H125 non-small cell lung cancer cells quantified by real-time PCR relative to rRNA.
Downregulation of Bcl-2 mRNA in human NCI-H125 non-small cell lung cancer cells quantified by real-time PCR relative to rRNA.
|
15625915 |
| NCI-H125 | IC50 |
80 nM
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Downregulation of Bcl-xL mRNA in human NCI-H125 non-small cell lung cancer cells quantified by real-time PCR relative to rRNA.
Downregulation of Bcl-xL mRNA in human NCI-H125 non-small cell lung cancer cells quantified by real-time PCR relative to rRNA.
|
15625915 |
In Vitro
ASO-5005 effectively downregulates the mRNA levels of Bcl-2 and Bcl-xL in MDA-MB-231 breast cancer cells, with an IC50 value of 65 nM for Bcl-2 and an IC50 value of 97 nM for Bcl-xL[1].
ASO-5005 (2 h)-mediated downregulation of Bcl-xL mRNA in MDA-MB-231 breast cancer cells is first detectable as early as 2 hours post-treatment and increases over time[1].
ASO-5005 downregulates Bcl-2 and Bcl-xL mRNA in H125 non-small cell lung cancer cells, with an IC50 value of 71 nM for Bcl-2 and an IC50 value of 80 nM for Bcl-xL[1].
ASO-5005 does not significantly alter the expression of the off-target genes Bcl-W, survivin, Akt and p53 in MDA-MB-231 breast cancer cells[1].
ASO-5005 (150-300 nM; 6 h of initial culture plus 42 h of culture after medium change, for a total of 48 h) reduces Bcl-2 and Bcl-xL protein levels in MDA-MB-231 breast cancer cells and H125 non-small cell lung cancer cells at concentrations of 150 nM and 300 nM[1].
ASO-5005 reduces the viability of MDA-MB-231 breast cancer cells and H125 non-small cell lung cancer cells, with morphological evidence of apoptosis[1].
ASO-5005 (50-100 nM; 72 h) sensitizes MDA-MB-231 breast cancer cells and H125 non-small cell lung cancer cells to a variety of anticancer agents, and reduces cell viability to a greater extent than single-agent treatment[1].
ASO-5005 (50-100 nM) induces caspase-3 activation and enhances chemotherapy-induced Caspase-3 activation in both MDA-MB-231 breast cancer cells and H125 non-small cell lung cancer cells[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 human breast cancer cells; NCI-H125 human non-small cell lung cancer cells
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Concentration:150 nM; 300 nM
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Incubation Time:6 hours initial incubation plus 42 hours post-medium renewal (total 48 hours)
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Result:Caused visible downregulation of both Bcl-2 and Bcl-xL protein in MDA-MB-231 cells at 150 nM and 300 nM.
Effectively inhibited Bcl-xL expression in MDA-MB-231 cells at 150 nM, whereas the 2'-MOE analog 4625 showed suboptimal Bcl-xL suppression at this concentration.
Downregulated both Bcl-2 and Bcl-xL protein in H125 cells.
Exhibited a superior effect on Bcl-xL protein downregulation in H125 cells compared with 4625.
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Cell Line:MDA-MB-231 human breast cancer cells; NCI-H125 human non-small cell lung cancer cells
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Concentration:50 nM; 100 nM (pretreatment)
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Incubation Time:Up to 72 hours after oligonucleotide addition
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Result:Reduced cell viability to below 50% in both cell lines when used as a single agent at low concentrations.
Reduced cell viability more strongly in combination with anticancer agents than either agent alone.
Produced the strongest reduction in cell viability in combination with paclitaxel in MDA-MB-231 cells.
Produced the strongest reduction in cell viability in combination with cisplatin and gemcitabine in H125 cells.
Showed a more obvious chemosensitization difference in H125 cells than in MDA-MB-231 cells.
Chemical Information
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SMILES
[ASO-5005]
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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)