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] .
For research use only. We do not sell to patients.
- CAS No.: 1313363-06-2
- Formula: C37H45ClN4O4
- Molecular Weight:645.24
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
Cellular Effect
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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] |
In Vitro
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. Further protocols information, click here.
Chemical Information
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CAS No. 1313363-06-2
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Molecular Weight 645.24
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Directly Induced Neuron Culture
Directly induced neuron culture converts somatic cells, most commonly fibroblasts, into induced neurons without passing through a pluripotent or neural progenitor stage; classic evidence shows that mouse fibroblasts can be converted by Ascl1, Brn2/Pou3f2, and Myt1l, human fibroblasts can be converted by defined neuronal transcription factors, and human fibroblasts can also be converted by miR-9/9-124 with neurogenic or subtype-specifying transcription factors. The readout is acquisition of neuronal identity and function, assessed by neuronal morphology, neuronal markers such as Tuj1/βIII-tubulin, MAP2, synapsin, and subtype markers when relevant, together with functional assays such as action-potential firing, synaptic activity, and electrophysiology.
Purity & Documentation
References
[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)