Milademetan HCl (1398568-47-2 free base)
| Code | Size | Price |
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| TAR-T28038-100mg | 100mg | Enquire | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Quantity:
| TAR-T28038-500mg | 500mg | Enquire | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Quantity:
Prices exclude any Taxes / VAT
Overview
Regulatory Status: RUO
Shipping:
cool pack
Storage:
-20°C
Documents
Further Information
Bioactivity:
Milademetan is a potent and selective MDM2 inhibitor. MDM2 inhibitor DS-3032b binds to and prevents the binding of MDM2 protein to the transcriptional activation domain of the tumor suppressor protein p53 upon oral administration. By preventing this MDM2-p53 interaction, the proteosome-mediated enzymatic degradation of p53 is inhibited and the transcriptional activity of p53 is restored. This results in the restoration of p53 signaling and leads to the p53-mediated induction of tumor cell apoptosis.
CAS:
T28038
Molecular Weight:
654.99
Purity:
0.98
SMILES:
O=C([C@H](N1)[C@H](C2=C(F)C(Cl)=NC=C2)[C@]3(C(NC4=C3C=CC(Cl)=C4)=O)C51CCC(C)(C)CC5)N[C@H]6CO[C@H](C(N)=O)CC6.[H]Cl
References
Liao G, Yang D, Ma L, Li W, Hu L, Zeng L, Wu P, Duan L, Liu Z. The development of piperidinones as potent MDM2-P53 protein-protein interaction inhibitors for cancer therapy. Eur J Med Chem. 2018 Nov 5;159:1-9. doi: 10.1016/j.ejmech.2018.09.044. Epub 2018 Sep 18. Review. PubMed PMID: 30253242.
Ishizawa J, Nakamaru K, Seki T, Tazaki K, Kojima K, Chachad D, Zhao R, Heese LE, Ma W, Ma MCJ, DiNardo CD, Pierce SA, Patel KP, Tse A, Davis RE, Rao A, Andreeff M. Predictive gene signatures determine tumor sensitivity to MDM2 inhibition. Cancer Res. 2018 Feb 28. pii: canres.0949.2017. doi: 10.1158/0008-5472.CAN-17-0949. [Epub ahead of print] PubMed PMID: 29490944.
Arnhold V, Schmelz K, Proba J, Winkler A, W?nschel J, Toedling J, Deubzer HE, K?nkele A, Eggert A, Schulte JH, Hundsdoerfer P. Reactivating TP53 signaling by the novel MDM2 inhibitor DS-3032b as a therapeutic option for high-risk neuroblastoma. Oncotarget. 2017 Dec 18;9(2):2304-2319. doi: 10.18632/oncotarget.23409. eCollection 2018 Jan 5. PubMed PMID: 29416773; PubMed Central PMCID: PMC5788641.