NVP-CFC218
NVP-CFC218 is a selective TP53-MDM2 inhibitor with a structure and biochemical profile similar to NVP-CGM097 (HY-15954) (IC50 of 1.6 nM: displacing the p53 peptide from the surface of HDM2). It is used to analyze pharmacological sensitivity in cell lines and is also applicable in cancer research [1] .
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- CAS No.: 1313363-06-2
- Formule: C37H45ClN4O4
- Masse moléculaire:645.24
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| SJSA-1 | GI50 |
0.35 μM
Compound: 12
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Inhibition of cell proliferation of human SJSA1 cells
Inhibition of cell proliferation of human SJSA1 cells
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[PMID: 26181851] |
NVP-CFC218 shows the same pattern of performance for the 13C-gene signature as NVP-CGM097 in 28 likely TP53 wild-type cancer cell lines and demonstrates a 51% response rate in 84 likely TP53 wild-type cancer cell lines[1].
NVP-CFC218 (30 min) potently inhibits p53–HDM2 interaction with high affinity and is substantially less active against p53–HDMX interaction (IC50 for HDM2 = 1.6 nM; IC50 for HDMX = 1300 nM)[2].
NVP-CFC218 inhibits proliferation of p53WT cell lines with higher potency than p53-null cell lines (GI50 for HCT116 p53WT = 473 nM; GI50 for SJSA-1 = 353 nM)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1313363-06-2
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Masse moléculaire 645.24
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Formule C37H45ClN4O4
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SMILES
O=C1N([C@H](C=2C(=CC(OC)=C(OC(C)C)C2)C1)C3=CC=C(Cl)C=C3)C4=CC=C(N(C[C@@H]5CC[C@H](CC5)N6CC(=O)NCC6)C)C=C4
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Sonkin D, et al. Expression signature based on TP53 target genes doesn't predict response to TP53-MDM2 inhibitor in wild type TP53 tumors. Elife. 2015;4:e10279. Published 2015 Oct 22. [Content Brief]
[2]. Jeay S, et al. A distinct p53 target gene set predicts for response to the selective p53-HDM2 inhibitor NVP-CGM097. Elife. 2015;4:e06498. Published 2015 May 12. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
NVP-CFC218 Related Classifications
HY-180331 Related Classifications
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