Contragestazol
Contragestazol (DL111-IT) is a non-hormonal antifertility agent. Contragestazol reduces the expression of Cyclin D1 and CDK4, increases the expression of total retinoblastoma protein (pRb), and decreases the level of hyperphosphorylated pRb. Contragestazol induces G0/G1 phase cell cycle arrest. Contragestazol inhibits embryonic development by inducing luteal cell apoptosis and reducing intrauterine polyamine levels. Contragestazol exhibits antitumor activity against prostate cancer, S180 tumor and H22 tumor. Contragestazol shows extremely potent activity in terminating early pregnancy in animals.
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- CAS. Nr.: 69095-83-6
- Formel: C17H17N3O
- Molecular Weight:279.34
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
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CDK4 |
Contragestazol (2.5-40 μg/mL; 48 h) inhibits the proliferation of 12 tested cancer cell lines (including P388, HO-8910 and A549) in a dose-dependent manner after 48 hours of treatment, with IC50 values ranging from 4.1 to 17.4 μg/mL[1].
Contragestazol (1.5-6.0 μg/mL; 24-144 h) inhibits the proliferation of HO-8910 ovarian cancer cells in a time-dependent manner[1].
Contragestazol (5.0-20.0 μg/mL; 48 h) induces dose-dependent G0/G1 cell cycle arrest in HO-8910 ovarian cancer cells after 48 h of exposure[1].
Contragestazol (5.0-20.0 μg/mL; 24 h) regulates the expression of cell cycle regulatory proteins in human HO-8910 ovarian cancer cells following 24 h of exposure, increases total pRb levels, decreases hyperphosphorylated pRb levels, and downregulates the expression of Cyclin D1 and CDK4 in a dose-dependent manner[1].
Contragestazol (DL111-IT) (2.5-40 µg/mL; 48 h) potently inhibits the proliferation of the androgen-independent prostate cancer cell line PC3 in vitro, with an IC50 of 9.9 µg/mL[2].
Contragestazol (DL111-IT) (5-20 µg/mL; 48 h) induces dose-dependent G0/G1 cell cycle arrest (without apoptosis) in the androgen-independent prostate cancer cell line PC3[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HO-8910, KB, HCT116, K562, CNE, RD, A549, Hela, HL60, PC3, Bel7402, P388
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Concentration:2.5 μg/mL, 5 μg/mL, 10 μg/mL, 20 μg/mL, 40 μg/mL
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Incubation Time:48 h
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Result:Induced dose-dependent sensitivity in all 12 tested cell lines.
Resulted in IC50 values ranging from 4.1 μg/mL (P388 cells) to 17.4 μg/mL (A549 cells).
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Cell Line:HO-8910
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Concentration:1.5 μg/mL, 6.0 μg/mL
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Incubation Time:24-144 h
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Result:Exerted mild cytotoxicity at 1.5 μg/mL and stronger cell killing activity in a time-dependent manner at 6.0 μg/mL.
Achieved proliferation inhibition rates of 20.5% (P<0.05) at 1.5 μg/mL and 41.0% (P<0.01) at 6.0 μg/mL after 144 h.
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Cell Line:HO-8910
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Concentration:5.0 μg/mL, 10.0 μg/mL, 20.0 μg/mL
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Incubation Time:48 h
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Result:Induced dose-dependent G0/G1 cell cycle arrest in HO-8910 cells.
Increased the percentage of cells in G0/G1 phase to 43.8% at 5.0 μg/mL, 66.2% at 10.0 μg/mL, and 76.2% at 20.0 μg/mL.
Decreased the proportion of cells in S phase in a dose-dependent manner.
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Cell Line:HO-8910
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Concentration:5.0 μg/mL, 10.0 μg/mL, 20.0 μg/mL
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Incubation Time:24 h
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Result:Increased total pRb protein levels in a dose-dependent manner.
Decreased hyperphosphorylated pRb levels in a dose-dependent manner.
Reduced Cyclin D1 and CDK4 protein expression at 10.0 and 20.0 μg/mL in a dose-dependent pattern.
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Cell Line:human androgen-independent prostate cancer cell line PC3
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Concentration:2.5 µg/mL, 5.00 µg/mL, 10.00 µg/mL, 20.00 µg/mL, 40.00 µg/mL
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Incubation Time:48 h
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Result:Dose-dependently inhibited PC3 cell proliferation.
Achieved an IC50 value of 9.9 µg/mL.
Contragestazol (DL111-IT) (12.5-50.0 mg/kg; intramuscular injection; once daily; for 9 consecutive days) dose-dependently inhibits the growth of H22 tumors in male ICR mice, with a tumor inhibition rate of 56.6% at the 50.0 mg/kg dose[1].
Contragestazol (DL111-IT) (12.5-50.0 mg/kg; intramuscular injection; 4 times per week; for 15 days) dose-dependently inhibits the growth of HO-8910 xenograft tumors in female Balb/c nude mice, with the tumor weight inhibition rate reaching 64.8% in the 50.0 mg/kg dose group[1].
Contragestazol (DL111-IT) (1.25-20.0 mg/kg; intramuscular injection; once daily; for 10 consecutive days) dose-dependently inhibits the growth of PC3 prostate cancer xenografts in female Balb/c athymic nude mice, with tumor weight inhibition rates ranging from 20.8% to 50.0% at doses of 1.25 mg/kg to 20.0 mg/kg, and does not affect the body weight of mice[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ICR (male)[1]
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Dosage:12.5 mg/kg; 25.0 mg/kg; 50.0 mg/kg
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Administration:i.m.; once daily; 9 consecutive days
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Result:Achieved a 33.6% tumor inhibition rate (S180).
Achieved a 50.0% tumor inhibition rate (S180).
Achieved a 55.9% tumor inhibition rate (S180).\n
Achieved a 24.5% tumor inhibition rate (H22).
Achieved a 52.0% tumor inhibition rate (H22).
Achieved a 56.6% tumor inhibition rate (H22).
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Animal Model:Balb/c athymic nude (female, 4- to 5-week-old)[1]
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Dosage:12.5 mg/kg; 25.0 mg/kg; 50.0 mg/kg
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Administration:i.m.; four times per week; 15 days
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Result:Achieved a 17.1% tumor weight inhibition rate (no statistical significance reported) and a 7.7-fold increase in tumor volume from baseline.
Achieved a 44.8% tumor weight inhibition rate (P<0.001), significant tumor volume inhibition starting at day 7 (P<0.01-0.001), and a 5.3-fold increase in tumor volume from baseline.
Achieved a 64.8% tumor weight inhibition rate (P<0.001), significant tumor volume inhibition starting at day 7 (P<0.01-0.001), and a 3.9-fold increase in tumor volume from baseline.
Caused no significant effect on mouse body weight for any dose.
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Animal Model:Balb/c (female, athymic nude, 4- to 5-week-old, subcutaneous injection of PC3 human prostate cancer cells)[2]
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Dosage:1.25 mg/kg; 5.0 mg/kg; 20.0 mg/kg
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Administration:i.m.; once daily; 10 days
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Result:Inhibited tumor volumes significantly (P < 0.05-0.01) in the 5.0 mg/kg and 20.0 mg/kg groups at day 4.
Reduced tumor growth rate (P < 0.05) in the 1.25 mg/kg group starting at day 6.
Increased tumor volumes 3.5-fold, 2.6-fold, and 2.0-fold in the 1.25 mg/kg, 5.0 mg/kg, and 20.0 mg/kg groups respectively by day 13, compared to 6.7-fold in control group.
Achieved tumor weight inhibition rates of 20.8% (1.25 mg/kg), 41.7% (5.0 mg/kg), and 50.0% (20.0 mg/kg).
Caused no significant changes in animal body weight across treatment groups.
Chemical Information
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CAS. Nr. 69095-83-6
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Molecular Weight 279.34
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Formel C17H17N3O
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SMILES
COC1=CC=CC(C2=NN=C(C3=C(CC)C=CC=C3)N2)=C1
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Synonyms
DL111-IT
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[1]. Yang B, et al. Antiproliferative activity of contragestazol (DL111-IT) in murine and human tumor models in vitro and in vivo. Cancer Chemother Pharmacol. 2006;57(2):268-273. [Content Brief]
[2]. He QJ, et al. Contragestazol (DL111-IT) inhibits proliferation of human androgen-independent prostate cancer cell line PC3 in vitro and in vivo. Asian J Androl. 2005 Dec;7(4):389-93. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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