
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)






Size | Price / USD | Stock | Quantity |
5MG | 1042 | Get Quote |
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50MG | 2124 | Get Quote |
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100MG | 3222 | Get Quote |
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200MG | Get Quote | Get Quote |
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500MG | Get Quote | Get Quote |
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1G | Get Quote | Get Quote |
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Biological Information
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Product NameDS-3032b
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NoteResearch use only, not for human use.
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Brief DescriptionDS-3032b is a potent, selective, orally available MDM2-p53 inhibitor with potential antineoplastic activity.
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DescriptionDS-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.
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In VitroMilademetan (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).
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In VivoMilademetan (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.
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SynonymsDS 3032b | DS3032b | Milademetan | DS 3032
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PathwayApoptosis
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TargetMDM2-p53
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RecptorMDM2-p53
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Research AreaCancer
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IndicationBlood cancer
Chemical Information
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CAS Number1398568-47-2
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Formula Weight618.531
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Molecular FormulaC30H34Cl2FN5O4
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Purity>98% (HPLC)
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SolubilityIn Vitro:?DMSO : 16.67 mg/mL (26.95 mM)
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SMILESCC1(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
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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
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1.?Ishizawa J, et al. Cancer Res. 2018 May 15;78(10):2721-2731.
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