CH4933468
CH4933468 is a thiohydantoin derivative, shows androgen receptor (AR) pure antagonist activity in vitro. CH4933468 inhibits AR-mediated transactivation and proliferation of LNCaP and LNCaP-BC2 cells. CH4933468 can be used for castration-resistant prostate cancer (CRPC) research.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 875055-92-8
- 分子式: C15H17ClN4O3S2
- 分子量:400.90
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CHO-K1 | IC50 |
440 nM
Compound: 32d
|
Displacement of [3H]mibolerone from human AR expressed in CHO-K1 cells after 2 hrs by scintillation counting
Displacement of [3H]mibolerone from human AR expressed in CHO-K1 cells after 2 hrs by scintillation counting
|
[PMID: 20381361] |
| HeLa | IC50 |
200 nM
Compound: 4, CH4933468
|
Antagonist activity at human AR expressed in human HeLa cells co-transfected with MMTV-Luc-Hyg after 48 hrs by transient-luciferase reporter gene assay
Antagonist activity at human AR expressed in human HeLa cells co-transfected with MMTV-Luc-Hyg after 48 hrs by transient-luciferase reporter gene assay
|
[PMID: 21050768] |
| LNCaP | IC50 |
10 nM
Compound: 4, CH4933468
|
Antagonist activity at AR in human bicalutamide-resistant LNCAP cells assessed as inhibition of cell proliferation after 6 days
Antagonist activity at AR in human bicalutamide-resistant LNCAP cells assessed as inhibition of cell proliferation after 6 days
|
[PMID: 21050768] |
| LNCaP | IC50 |
12 nM
Compound: 32d
|
Antagonist activity at AR in bicalutamide-resistant human LNCAP cells assessed as effect on cell proliferation after 6 days
Antagonist activity at AR in bicalutamide-resistant human LNCAP cells assessed as effect on cell proliferation after 6 days
|
[PMID: 20381361] |
| LNCaP | IC50 |
410 nM
Compound: 32d
|
Antagonist activity at AR in human LNCAP cells assessed as effect on cell proliferation after 6 days
Antagonist activity at AR in human LNCAP cells assessed as effect on cell proliferation after 6 days
|
[PMID: 20381361] |
| LNCaP | IC50 |
410 nM
Compound: 67; CH4933468
|
Antiproliferative activity against human LNCaP cells
Antiproliferative activity against human LNCaP cells
|
[PMID: 35786895] |
化学情報
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CAS 番号 875055-92-8
-
分子量 400.90
-
分子式 C15H17ClN4O3S2
-
SMILES
O=S(CCCN(C(N1C2=CC=C(C#N)C(Cl)=C2)=S)C(C)(C)C1=O)(N)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
-
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
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)