DS-3032b

CAS No. 1398568-47-2

DS-3032b( DS 3032b | DS3032b | Milademetan | DS 3032 )

Catalog No. M11665 CAS No. 1398568-47-2

DS-3032b is a potent, selective, orally available MDM2-p53 inhibitor with potential antineoplastic activity.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
5MG 1042 Get Quote
50MG 2124 Get Quote
100MG 3222 Get Quote
200MG Get Quote Get Quote
500MG Get Quote Get Quote
1G Get Quote Get Quote

Biological Information

  • Product Name
    DS-3032b
  • Note
    Research use only, not for human use.
  • Brief Description
    DS-3032b is a potent, selective, orally available MDM2-p53 inhibitor with potential antineoplastic activity.
  • Description
    DS-3032b is a potent, selective, orally available MDM2-p53 inhibitor with potential antineoplastic activity; binds to, and prevents the binding of MDM2 protein to the transcriptional activation domain of the tumor suppressor protein p53; restores p53 signaling and leads to the p53-mediated induction of tumor cell apoptosis.Blood Cancer Phase 1 Clinical.
  • In Vitro
    Milademetan (DS-3032) can stabilize TP53 and selectively induce CDKNA1, BAX and MDM2 expression in neuroblastoma cells with wild-type TP53.Milademetan (DS-3032b) treatment enhances TP53 target gene expression and induces G1 cell cycle arrest, senescence and apoptosis.Milademetan (DS-3032b, 0-2000 nM) treatment selectively inhibits viability, proliferation and migration of neuroblastoma cells with wildtype TP53 independently of MYCN status. Cell Viability Assay Cell Line:SK-N-SH, SH-SY5Y, IMR32, IMR5 and LAN5 cell lines.Concentration:0-2000 nM.Incubation Time:24-72 h.Result:Reduced viability in a dose- and time-dependent manner.Exhibited IC50 values of 21.9 nM, 17.7 nM, 52.63 nM, 25.7 nM and 44.1 nM in SK-N-SH, SH-SY5Y, IMR32, IMR5 and LAN5 cell lines, respectively (72 h).
  • In Vivo
    Milademetan (DS-3032b, 50 mg/kg, oral gavage) delays tumor growth and improves survival in mice xenografted with neuroblastoma cells with functional TP53. Animal Model:SH-SY5Y xenograft tumors in nude mice.Dosage:50mg/kg. Administration:Oral gavage for 30 consecutive days with an alternating schedule of 4 days of daily treatment with oral gavages followed by 2 days without treatment (4+2).Result:Survival in the mouse cohort was significantly prolonged.Reduced neuroblastoma xenograft tumor growth by activating TP53 signaling.
  • Synonyms
    DS 3032b | DS3032b | Milademetan | DS 3032
  • Pathway
    Apoptosis
  • Target
    MDM2-p53
  • Recptor
    MDM2-p53
  • Research Area
    Cancer
  • Indication
    Blood cancer

Chemical Information

  • CAS Number
    1398568-47-2
  • Formula Weight
    618.531
  • Molecular Formula
    C30H34Cl2FN5O4
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 16.67 mg/mL (26.95 mM)
  • SMILES
    CC1(CCC2(CC1)C3(C(C(N2)C(=O)NC4CCC(OC4)C(=O)N)C5=C(C(=NC=C5)Cl)F)C6=C(C=C(C=C6)Cl)NC3=O)C
  • Chemical Name
    (3'R,4'S,5'R)-N-((3S,6R)-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

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1.?Ishizawa J, et al. Cancer Res. 2018 May 15;78(10):2721-2731.
molnova catalog
related products
  • MB725

    MB725 is a small-molecule p53 mutant Y220C stabilizer, induces selective viability reduction in several p53-Y220C cancer cell lines (Huh7 cell IC50=10 uM).

  • p53-Mdm2 inhibitor 4

    p53-Mdm2 inhibitor 4 inhibits the p53-MDM2 protein-protein interaction.

  • HL001

    HL001 (HL 001) is a potent cyclophilin A (CypA) inhibitor with IC50 of 31.6 nM.