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.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- CAS No.: 849723-20-2
- 화학식: C24H22ClNO3
- 분자량:407.89
-
보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
|
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] |
Chemical Information
-
CAS No. 849723-20-2
-
분자량 407.89
-
화학식 C24H22ClNO3
-
SMILES
O=C1N(CC2=CC=CC=C2)C(OCCCO)(C3=CC=C(Cl)C=C3)C4=C1C=CC=C4
-
선적
Room temperature in continental US; may vary elsewhere.
-
보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)