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.
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
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Biological Activity
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Chemical Information
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Biological Activity
Description
IC50 & Target
[1]|
BCL2 |
In Vitro
G4232 (400 nM; 5 h transfection, 67 h post-incubation, total 72 h) does not induce significant apoptosis in DU145 prostate cancer cells with either mock transfection or AS1 bcl-2 knockdown[2].
G4232 exerts minimal effects on cell cycle progression in both mock-transfected and AS1 bcl-2 knockdown DU145 prostate cancer cells, and only causes a moderate increase in S-phase cells that fail to incorporate BrdUrd[2].
G4232 (400 nM; 3 days) induces only minimal reactive oxygen species production in mock-transfected, AS1, and AS2 DU145 prostate cancer cells[2].
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
Intraperitoneal bolus administration of G4232 (5 mg/kg/day; i.p.; daily bolus injection; 14 days) produces equivalent antitumor activity, Bcl-2 downregulation, and apoptosis induction as continuous subcutaneous infusion in the melanoma xenograft model[1].
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.
Chemical Information
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SMILES
[G4232]
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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)
G4232 Related Classifications
HY-118874H Related Classifications
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