Onapristone
Onapristone is a progesterone receptor antagonist, with Kds of 11.6 nM and 11.90 nM for human endometrium and myometrium progesterone receptor in saturation analysis. Onapristone has antitumor activity.
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- CAS 番号: 96346-61-1
- 分子式: C29H39NO3
- 分子量:449.62
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
Kd: 1.6 nM (Human endometrium progesterone receptor), 11.90 nM (Human myometrium progesterone receptor)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CV-1 | EC50 |
2.2 nM
Compound: Onapristone
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Antagonistic activity at human progesterone receptor in CV-1 cells.
Antagonistic activity at human progesterone receptor in CV-1 cells.
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[PMID: 12781198] |
| CV-1 | IC50 |
1.6 nM
Compound: ZK-98299
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Concentration required to give half-maximal inhibition against human Progesterone receptor B isoform in co-transfected CV-1 cell lines.
Concentration required to give half-maximal inhibition against human Progesterone receptor B isoform in co-transfected CV-1 cell lines.
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[PMID: 8627601] |
| CV-1 | IC50 |
2.2 nM
Compound: 2
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Antagonist activity against human progesterone receptor (hPR) using cotransfection assay in CV-1 cells
Antagonist activity against human progesterone receptor (hPR) using cotransfection assay in CV-1 cells
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[PMID: 10743938] |
| T47D | IC50 |
3.3 nM
Compound: 2
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Antagonist activity against human progesterone receptor (hPR) in T47D human breast cancer cell line
Antagonist activity against human progesterone receptor (hPR) in T47D human breast cancer cell line
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[PMID: 10743938] |
| T47D | IC50 |
3.3 nM
Compound: Onapristone
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Inhibition of human progesterone receptor activation in T47D human breast cancer cell.
Inhibition of human progesterone receptor activation in T47D human breast cancer cell.
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[PMID: 12781198] |
Onapristone is a progesterone receptor antagonist, with Kds of 11.6 nM and 11.90 nM for human endometrium and myometrium progesterone receptor in saturation analysis. In Scatchard analysis, Onapristone shows Kds of 9.80 nM and 15.42 nM for human endometrium and myometrium progesterone receptor[1]. Onapristone (16, 64 μM) reduces the viability of ISHIKAWA cells after treatment for 96 h. Onapristone (20 μM) also induces ISHIKAWA cell apoptosis after treatment for 72 h. However, Onapristone shows no inhibition on HEC1A and SKUT2 cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 96346-61-1
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分子量 449.62
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分子式 C29H39NO3
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SMILES
C[C@]12[C@](CC[C@]2(O)CCCO)([H])[C@@]3([H])C([C@@H](C4=CC=C(N(C)C)C=C4)C1)=C5C(CC3)=CC(CC5)=O
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別名
ZK 98299
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[1]. Puri CP, et al. Binding characteristics of progesterone and antiprogestin ZK 98.299 in human endometrial and myometrial cytosol. Biochim Biophys Acta. 1989 May 10;1011(2-3):176-82. [Content Brief]
[2]. Huang Y, et al. Inhibiting Nuclear Phospho-Progesterone Receptor Enhances Antitumor Activity of Onapristone in Uterine Cancer. Mol Cancer Ther. 2018 Feb;17(2):464-473. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Onapristone 関連分類
HY-106389 関連分類
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