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] [2].

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 p53^WT cell lines with higher potency than p53-null cell lines (GI₅₀ for HCT116 p53^WT = 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.

645.24

C₃₇H₄₅ClN₄O₄

1313363-06-2

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

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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]