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] .
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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: 1313363-06-2
- 分子式: C37H45ClN4O4
- 分子量:645.24
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| SJSA-1 | GI50 |
0.35 μM
Compound: 12
|
Inhibition of cell proliferation of human SJSA1 cells
Inhibition of cell proliferation of human SJSA1 cells
|
[PMID: 26181851] |
体外実験
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.
化学情報
-
CAS 番号 1313363-06-2
-
分子量 645.24
-
分子式 C37H45ClN4O4
-
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
-
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.
プロトコル
-
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.
-
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.
純度とドキュメンテーション
参考文献
[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
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)