Oblimersen
Oblimersen is a BCL-2 inhibitor targeting BCL-2 RNA. Oblimersen specifically binds to the first six codons of the bcl-2 mRNA sequence, resulting in degradation of bcl-2 mRNA and induces apoptosis by down-regulating expression of Bcl-2. Oblimersen can be used for cancer research.
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- CAS No.: 190977-41-4
- Masse moléculaire:5684.61
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Oblimersen (500 nM; 72 hours; human small-cell lung cancer cell lines H69) decreases BCL-2 protein expression in vitro[1].
Oblimersen (500 nM; 72 hours; human small-cell lung cancer cell lines H69) increases radiation-induced apoptosis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human small-cell lung cancer cell lines H69
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Concentration:500 nM
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Incubation Time:72 hours
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Result:Decreased BCL-2 protein levels.
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Cell Line:Human small-cell lung cancer cell lines H69
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Concentration:500 nM
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Incubation Time:72 hours
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Result:Arrested cell cycle at sub G1 phase.
Oblimersen (5-10 mg/kg; i.p.; daily (Monday to Friday), for 3 weeks) has antitumor efficacy in the subcutaneous tumor model[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male severe combined immunodeficient (SCID)-RAG2 mice[2]
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Dosage:5 and 10 mg/kg
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Administration:Intraperitoneal injection; daily (Monday to Friday), for 3 weeks
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Result:Inhibited tumor growth in a dose-dependent manner.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 190977-41-4
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Masse moléculaire 5684.61
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SMILES
[Oblimersen]
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Sequence
DNA, d(P-thio)(T-C-T-C-C-C-A-G-C-G-T-G-C-G-C-C-A-T)
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Loriot Y, et, al. Inhibition of BCL-2 in small cell lung cancer cell lines with oblimersen, an antisense BCL-2 oligodeoxynucleotide (ODN): in vitro and in vivo enhancement of radiation response. Anticancer Res. 2010 Oct;30(10):3869-78. [Content Brief]
[2]. Hu Y, et, al. Antitumor efficacy of oblimersen Bcl-2 antisense oligonucleotide alone and in combination with vinorelbine in xenograft models of human non-small cell lung cancer. Clin Cancer Res. 2004 Nov 15;10(22):7662-70. [Content Brief]
[3]. Klasa RJ, et, al. Oblimersen Bcl-2 antisense: facilitating apoptosis in anticancer treatment. Antisense Nucleic Acid Drug Dev. 2002 Jun;12(3):193-213. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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