NU-8165
NU-8165 is an inhibitor of the MDM2-p53 protein-protein interaction with anti-tumor activity. Optimization of NU-8165 was guided by MDM2 NMR titrations, which indicated key binding interaction regions. NU-8165 activated MDM2 and p21 transcription in cell-based assays and showed modest selectivity for wild-type p53 cell lines.
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- CAS 番号: 849723-20-2
- 分子式: C24H22ClNO3
- 分子量:407.89
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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 |
|---|---|---|---|---|
| HCT-116 | GI50 |
79 μM
Compound: 4a
|
Growth inhibition of human HCT116 cells harboring p53+/+ after 48 hrs by Hoechst 33258 staining based fluorescence assay
Growth inhibition of human HCT116 cells harboring p53+/+ after 48 hrs by Hoechst 33258 staining based fluorescence assay
|
[PMID: 29089230] |
| HCT-116 | GI50 |
90 μM
Compound: 4a
|
Growth inhibition of human p53 knockdown HCT116 cells after 48 hrs by Hoechst 33258 staining based fluorescence assay
Growth inhibition of human p53 knockdown HCT116 cells after 48 hrs by Hoechst 33258 staining based fluorescence assay
|
[PMID: 29089230] |
| SJSA-1 | IC50 |
15.9 μM
Compound: 2c
|
Inhibitory concentration against MDM2-p53 interaction in SJSA human sarcoma cells
Inhibitory concentration against MDM2-p53 interaction in SJSA human sarcoma cells
|
[PMID: 15713419] |
化学情報
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CAS 番号 849723-20-2
-
分子量 407.89
-
分子式 C24H22ClNO3
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SMILES
O=C1N(CC2=CC=CC=C2)C(OCCCO)(C3=CC=C(Cl)C=C3)C4=C1C=CC=C4
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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)