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Art. -Nr.: HY-118874H

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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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Speicherung:

-20°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

G4232 Chemical Structure

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
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Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

BCL2

Alle Bcl-2 Family Isoform-spezifische Produkte anzeigen :

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen :

In Vitro

Anti-cancerApoptosisCell Cycle RegulationOxidative Stress

Anti-cancer

Apoptosis

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].

Anti-cancer

Cell Cycle Regulation

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].

Anti-cancer

Oxidative Stress

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.

Apoptosis Analysis^[2]

Cell Line:

mock-transfected and AS1 (bcl-2 antisense RNA) DU145 prostate cancer cells
Concentration:

400 nM (complexed with Lipofectin)
Incubation Time:

5 h transfection, 67 h post-incubation, total 72 h
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

Anti-cancerApoptosisCytokines & Chemokines

Anti-cancer

Apoptosis

Cytokines & Chemokines

G4232 (5 mg/kg/day; s.c.; continuous infusion via miniosmotic pump; 14 days) reduces melanoma xenograft tumor growth by approximately 40%, downregulates Bcl-2 expression by 60%, and increases tumor cell apoptosis to 3.6% in SCID mice^[1].

Anti-cancer

Apoptosis

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.

Animal Model:

C.B-17 scid/scid (SCID) mice (female; 4-6 weeks old; pathogen-free; 518A2 human melanoma cells xenotransplanted subcutaneously)^[1]
Dosage:

5 mg/kg/day
Administration:

s.c.; continuous infusion via miniosmotic pump; 14 days
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.

Animal Model:

C.B-17 scid/scid (SCID) mice (female; 4-6 weeks old; pathogen-free; 518A2 human melanoma cells xenotransplanted subcutaneously)^[1]
Dosage:

5 mg/kg/day
Administration:

i.p.; daily bolus injection; 14 days
Result:

Showed equally potent Bcl-2 downregulation, induction of apoptosis, and antitumor activity as observed with continuous s.c. administration.
Was well tolerated.

Related Protocols :

Chemical Information

Appearance Solid
SMILES

[G4232]
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

-20°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Reinheit & Dokumentation

Handling Instructions (2242 KB)

Verweise

[1]. Wacheck V, et al. Antitumor effect of G3139 Bcl-2 antisense oligonucleotide is independent of its immune stimulation by CpG motifs in SCID mice. Antisense & nucleic acid drug development. 2002 Dec;12(6):359-67.

[2]. Raffo A, et al. Antisense RNA down-regulation of bcl-2 expression in DU145 prostate cancer cells does not diminish the cytostatic effects of G3139 (Oblimersen). Clinical cancer research : an official journal of the American Association for Cancer Research. 2004 May 01;10(9):3195-206.

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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G4232

Alle Bcl-2 Family Isoform-spezifische Produkte anzeigen

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen

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