G4232
G4232 is an immune-silent BCL2 antisense oligonucleotide that binds to BCL2 mRNA to induce target degradation and inhibit Bcl-2 protein translation. G4232 carries 5'-methylcytosine in its two CpG motifs, which eliminates CpG-mediated immunostimulatory activity and does not cause significant splenomegaly or elevated plasma IL-12 levels in SCID mice. G4232 induces Apoptosis. G4232 inhibits tumor growth in a melanoma xenograft model. G4232 can be used in studies of melanoma and prostate cancer.
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Almacenamiento:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
BCL2 |
In Vitro
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:mock-transfected and AS1 (bcl-2 antisense RNA) DU145 prostate cancer cells
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Concentration:400 nM (complexed with Lipofectin)
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Incubation Time:5 h transfection, 67 h post-incubation, total 72 h
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Result:Induced 1.0% necrotic cells, 14.1% late apoptosis/early necrosis cells, 58.5% viable cells, and 26.4% early apoptotic cells in mock-transfected DU145 cells.
Induced 0.5% necrotic cells, 16.1% late apoptosis/early necrosis cells, 51.6% viable cells, and 31.8% early apoptotic cells in AS1 DU145 cells.
Produced relatively small numbers of apoptotic cells in both mock and AS1 cells, similar to other 18mer oligonucleotides examined.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C.B-17 scid/scid (SCID) mice (female; 4-6 weeks old; pathogen-free; 518A2 human melanoma cells xenotransplanted subcutaneously)[1]
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Dosage:5 mg/kg/day
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Administration:s.c.; continuous infusion via miniosmotic pump; 14 days
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Result:Reduced tumor growth by approximately 40% compared with saline-treated animals.
Led to a 60% relative reduction in xenotransplant Bcl-2 protein expression relative to saline control.
Did not significantly affect Bcl-xL protein expression.
Increased the percentage of apoptotic cells in tumor xenotransplants to 3.6%, compared with 0.8% in saline-treated mice.
Spleen weight was 139% relative to saline controls.
IL-12 serum levels were slightly elevated above saline levels but did not reach statistical significance.
Mean IL-6 serum level was 61 pg/mL.
Was well tolerated, with no apparent signs of toxicity or weight loss.
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Animal Model:C.B-17 scid/scid (SCID) mice (female; 4-6 weeks old; pathogen-free; 518A2 human melanoma cells xenotransplanted subcutaneously)[1]
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Dosage:5 mg/kg/day
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Administration:i.p.; daily bolus injection; 14 days
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Result:Showed equally potent Bcl-2 downregulation, induction of apoptosis, and antitumor activity as observed with continuous s.c. administration.
Was well tolerated.
- RNA extraction experimental
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Annexin V plus membrane-impermeant dye apoptosis staining
- Patient-Derived Xenograft (PDX)
- Apoptosis Solutions
- Patient-Derived Orthotopic Xenograft (PDOX)
- Splenic/Portal-Vein Liver Metastasis Xenograft
- Subcutaneous Cell-Line-Derived Xenograft
- Orthotopic Cell-Line Xenograft
- Intraperitoneal/Peritoneal Dissemination Xenograft
Chemical Information
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Appearance Solid
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SMILES
[G4232]
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
G4232 Related Classifications
HY-118874H Related Classifications
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