Milademetan free base
Milademetan, also known as DS-3032b or DS-3032, is a potent and selective MDM2 inhibitor with potential antineoplastic activity. Upon oral administration, MDM2 inhibitor DS-3032b binds to, and prevents the binding of MDM2 protein to the transcriptional activation domain of the tumor suppressor protein p53. 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.
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化学信息
| 名称 | Milademetan free base |
|---|---|
| Iupac 化学名称 | (3'R,4'S,5'R)-N-[(3R,6S)-6-carbamoyloxan-3-yl]-6''-chloro-4'-(2-chloro-3-fluoropyridin-4-yl)-4,4-dimethyl-2''-oxo-1'',2''-dihydrodispiro[cyclohexane-1,2'-pyrrolidine-3',3''-indole]-5'-carboxamide |
| 同义词 | DS-3032B; DS 3032B; DS3032B; DS-3032; DS 3032; DS3032; Milademetan free base; |
| 英文同义词 | DS-3032B; DS 3032B; DS3032B; DS-3032; DS 3032; DS3032; Milademetan free base; |
| 分子式 | C30H34Cl2FN5O4 |
| 分子量 | 618.53 |
| Smile | 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 |
| InChiKey | RYAYYVTWKAOAJF-QISPRATLSA-N |
| InChi | InChI=1S/C30H34Cl2FN5O4/c1-28(2)8-10-29(11-9-28)30(18-5-3-15(31)13-19(18)37-27(30)41)21(17-7-12-35-24(32)22(17)33)23(38-29)26(40)36-16-4-6-20(25(34)39)42-14-16/h3,5,7,12-13,16,20-21,23,38H,4,6,8-11,14H2,1-2H3,(H2,34,39)(H,36,40)(H,37,41)/t16-,20+,21+,23-,30-/m1/s1 |
| Cas号 | 1398568-47-2 |
| 相关CAS号 |
订购信息
| 包装 | 价格 | 库存 | 纯度 | 备货期 |
|---|---|---|---|---|
| 大货 | 询价 | 询价 | 询价 |
| 外观性状 | 固体粉末 |
|---|---|
| 纯度 | 98% Min. |
| 存储 | 短期（几天到几周）为0-4摄氏度，长期（几个月）为-20摄氏度 |
| 可溶性 | 溶于DMSO |
| 处理方式 | |
| 运输条件 | 作为非危险化学品在环境温度下装运。这种产品在正常运输和海关工作期间可以稳定几周. |
| 海关编码 |
| Targets | |
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| Mechanism | |
| Cell study | |
| Animal study | |
| Clinical study |
1: 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. 2: Arnhold V, Schmelz K, Proba J, Winkler A, Wünschel J, Toedling J, Deubzer HE, Künkele 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. 3. 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.
