Milademetan tosylate

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MedKoo CAT#: 206063

CAS#: 1398569-75-9 (tosylate)

Description: 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.

Chemical Structure

Milademetan tosylate
CAS# 1398569-75-9 (tosylate)

Theoretical Analysis

MedKoo Cat#: 206063
Name: Milademetan tosylate
CAS#: 1398569-75-9 (tosylate)
Chemical Formula: C37H42Cl2FN5O7S
Exact Mass:
Molecular Weight: 790.73
Elemental Analysis: C, 56.20; H, 5.35; Cl, 8.97; F, 2.40; N, 8.86; O, 14.16; S, 4.05

Size Price Shipping out time Quantity
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Pricing updated 2021-02-28. Prices are subject to change without notice.

DS-3032b tosylate is not in stock, but may be available through custom synthesis. For cost-effective reason, minimum 1 gram order is requested. The product will be characterized by NMR, HPLC and MS analysis. Purity (HPLC) is usually >98%. CoA, QC data, MSDS will be provided when product is successfully made. The estimated lead time is 2-3 months. Please send email to to inquire quote.

Related CAS #: 1398568-47-2 (free base)   1398569-75-9 (tosylate)   2095625-97-9 (tosylate hydrate)   Milademetan HCl    

Synonym: DS3032b; DS-3032b; DS 3032b; DS3032; DS-3032; DS 3032; DS-3032b tosylate; Milademetan tosylate

IUPAC/Chemical Name: (3'R,4'S,5'R)-N-((3R,6S)-6-carbamoyltetrahydro-2H-pyran-3-yl)-6''-chloro-4'-(2-chloro-3-fluoropyridin-4-yl)-4,4-dimethyl-2''-oxodispiro[cyclohexane-1,2'-pyrrolidine-3',3''-indoline]-5'-carboxamide tosylate


InChi Code: InChI=1S/C30H34Cl2FN5O4.C7H8O3S/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;1-6-2-4-7(5-3-6)11(8,9)10/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);2-5H,1H3,(H,8,9,10)/t16-,20+,21+,23-,30-;/m1./s1

SMILES Code: 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.OS(=O)(C7=CC=C(C)C=C7)=O

Solid powder

>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Soluble in DMSO, not soluble in water.

Shelf Life:
>5 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code:

Handling Instructions:

Preparing Stock Solutions

The following data is based on the product molecular weight 790.73 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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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.

Additional Information

 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. MDM2, a zinc finger protein and a negative regulator of the p53 pathway, is overexpressed in cancer cells; it has been implicated in cancer cell proliferation and survival.