Telapristone acetate
Telapristone acetate (CDB-4124) is a potent progesterone receptor (PR) modulator. Telapristone acetate inhibits the proliferation of ovarian cancer cells by inducing cell cycle arrest and apoptosis. Telapristone effectively inhibits the occurrence and development of spontaneous and chemically induced mammary tumors in rats. Telapristone acetate can be used for breast and ovarian cancer research.
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- CAS. Nr.: 198414-31-2
- Formel: C31H39NO5
- Molecular Weight:505.65
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Speicherung:
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Biologische Aktivität
IC50：35.5±3.9,21.3±1.8,43.6±5.1,47.4±3.9 μM of IGROV-1, IGROV-1 PTES, SKOV-3, SKOV-3 PTES cells, respectively[1].
Telapristone acetate (0-60 μM, 96 h) inhibits the growth of ovarian cancer cells resistant to Cisplatin (CDDP) (HY-17394) and Paclitaxel (PTX) (HY-B0015), with IC50 values of 35.5 μM (IGROV-1), 21.3 μM (IGROV-1 PTES), 43.6 μM (SKOV-3) and 47.4 μM (SKOV-3 PTES)[1].
Telapristone acetate (30 μM, 48 h) induces cell cycle arrest and apoptosis in IGROV-1 and IGROV-1 PTES cells, as evidenced by the upregulation of p21Cip1/p27Kip1 and PARP cleavage, respectively[1].
Telapristone acetate (0-10 μmol/L, 3-6 days) induces G1/S cell cycle arrest and thereby inhibits cell growth by downregulating CDK2 and CDK4 in human T47D cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human T47D cells
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Concentration:1 μmol/L
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Incubation Time:3 and 6 days
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Result:Failed to affect the expression of PRA ,PRB, cyclin D1, or CDK6.
Decreased ERα expression.
Decreased CDK2 and CDK4 expressions.
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Cell Line:IGROV-1, IGROV-1 PTES, SKOV-3, and SKOV-3 PTES
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Concentration:0, 7.5, 15, 30 and 60 μM
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Incubation Time:96 h
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Result:Reduced the viability of IGROV-1, IGROV-1 PTES, SKOV-3, and SKOV-3 PTES cells in a dose-dependent manner.
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Cell Line:IGROV-1 and IGROV-1 PTES
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Concentration:30 μM
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Incubation Time:48 h
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Result:Caused an increase in the abundance of the cell cycle inhibitor p27kip1 in both parental and PTES cells.
Increased cyclin dependent kinase inhibitor p21cip1, cell cycle arrest associated protein.
Showed no significant differences in the expression of G1 regulatory proteins CDk2 and cyclin E between parental and PTES cells.
Induced the cleavage of PARP, indicating it induces cell apopotosis.
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Cell Line:human T47D cells
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Concentration:0, 0.1, 1.0 and 10 μmol/L
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Incubation Time:3 and 6 days
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Result:Did not affect cell growth after either 3 days or 6 days of treatment at 0.1 μmol/L.
Suppressed cell growth in a dose-dependent manner at 1.0 and 10 μmol/L.
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Cell Line:human T47D cells
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Concentration:0.1, 1.0 and 10 μmol/L
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Incubation Time:3 and 6 days
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Result:Decreased the percentage of cells in S phase from 12.2% (control) to 8.5% after 3 days.
Decreased the percentage of cells in S phase from 14.1% (control) to 9.3% after 6 days.
Significant increased the proportion of cells in the G1/G0 phase after 6 days.
Inhibited the transition of cells from G1 to S phase of the cell cycle.
Telapristone acetate (3 and 30 mg/pellet, s.c., over 84 days, initiated 6 days post-MNU) suppresses the development of precancerous lesions and carcinogen-induced estrogen receptor (ER)+ mammary tumors in rats[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female SD rats[2]
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Dosage:20, 70, and 200 mg/kg
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Administration:i.g., daily for 24 months
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Result:Showed no significant changes at 20 and 70 mg/kg doses.
Slightly decreased the body weight (12.5%) at 200 mg/kg but the difference with control group was not significant.
Exhibited no substantial differences in tumors or other pathologies in internal organs (liver, spleen, heart, lung, intestine, brain, kidneys), compared to control.
Decreased fibroadenomas and hyperplastic lesions with atypia.
Increase cystic formations and induced calcifications among mammary gland parenchyma.
Reduced ductal lateral branching that leads to reduction in lobular structures in mammary gland.
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Animal Model:Female SD rats (50 days old) intraperitoneally injected with N-methyl-N-nitrosourea (MNU)[2]
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Dosage:3.0 and 30.0 mg/pellet
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Administration:s.c., over 84 days, initiated 6 days post-MNU
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Result:Significantly decreased the percentage of Ki-67-positive cells from 16.5% (control) to 9.1%.
Suppressed cell proliferation and induces apoptosis.
Showed average tumor latency of 74 days for the low-dose and 87 days for the high-dose.
Suppressed the incidence and multiplicity of mammary tumors in a dose-dependent manner.
Decreased tumor incidence from 85% (control) to 60% (low dose) and 35% (high dose).
Decreased tumor multiplicity, from 3.0 tumors/rat in the control group to 2.2 and 1.1 tumors/rat in the low- and high-dose, respectively.
Resulted in an increase in intercellular spaces between tumor cells and the development of cystic formations. Decreased serum progesterone, but had no effect on estradiol.
Suppressed PR expression in mammary tumors.
Showed no significant changes in animal body weight.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 198414-31-2
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Molecular Weight 505.65
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Formel C31H39NO5
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SMILES
C[C@@]12[C@](CC[C@]2(OC(C)=O)C(COC)=O)([H])[C@@]3([H])C([C@@H](C4=CC=C(N(C)C)C=C4)C1)=C(CC5)C(CC3)=CC5=O
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Synonyms
CDB-4124
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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]. Carlos D Gamarra-Luques,et al. Resistance to cisplatin and paclitaxel does not affect the sensitivity of human ovarian cancer cells to antiprogestin-induced cytotoxicity. J Ovarian Res. 2014 Apr 27;7:45. [Content Brief]
[2]. Wiehle R, et al. CDB-4124, a progesterone receptor modulator, inhibits mammary carcinogenesis by suppressing cell proliferation and inducing apoptosis. Cancer Prev Res (Phila). 2011 Mar;4(3):414-24. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Telapristone acetate Related Classifications
HY-16483 Related Classifications
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