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Milademetan

Product Name: Milademetan
CAS No.: 1398568-47-2
Chemical Name: Milademetan
Synonyms: DS-3032;Milademetan;Milademetan (DS-3032);DS-3032B (Milademetan);Milademetan, 10 mM in DMSO;DS-3032 (MILADEMETAN) (DS-3032B);(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;L-erythro-Hexonamide, 2,6-anhydro-5-[[[(3'R,4'S,5'R)-6''-chloro-4'-(2-chloro-3-fluoro-4-pyridinyl)-1'',2''-dihydro-4,4-dimethyl-2''-oxodispiro[cyclohexane-1,2'-pyrrolidine-3',3''-[3H]indol]-5'-yl]carbonyl]amino]-3,4,5-trideoxy-
CBNumber: CB14796670
Molecular Formula: C30H34Cl2FN5O4
Formula Weight: 618.53
MOL File: 1398568-47-2.mol

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Milademetan Property

Boiling point:: 840.7±65.0 °C(Predicted)
Density: 1.44±0.1 g/cm3(Predicted)
storage temp.: Store at -20°C
solubility: Soluble in DMSO
form: Solid
pka: 12.43±0.70(Predicted)
color: White to light yellow

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

ChemScene

Product number: CS-0021065
Product name: Milademetan
Purity: 98.16%
Packaging: 1mg
Price: $220
Updated: 2021/12/16

ChemScene

Product number: CS-0021065
Product name: Milademetan
Purity: 98.16%
Packaging: 5mg
Price: $660
Updated: 2021/12/16

ChemScene

Product number: CS-0021065
Product name: Milademetan
Purity: 98.16%
Packaging: 10mg
Price: $1100
Updated: 2021/12/16

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Milademetan Chemical Properties,Usage,Production

Uses

Milademetan (DS-3032) is a specific and orally active MDM2 inhibitor for the research of acute myeloid leukemia (AML) or solid tumors. Milademetan (DS-3032) induces G1 cell cycle arrest, senescence and apoptosis[1][2].

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^[4].

Animal Model:	SH-SY5Y xenograft tumors in nude mice^[4].
Dosage:	50 mg/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.

References

[1] ARYL SULFONOHYDRAZIDES. WO 2017069289 A1.
[2] M.M. Gounder, et al. Milademetan, an oral MDM2 inhibitor, in well-differentiated/dedifferentiated liposarcoma: results from a phase 1 study in patients with solid tumors or lymphomas. European Journal of Cancer 138S2 (2020) S1–S62.
[3] Li, Yangbing, et al. Development of novel PROTAC Small-Molecule Degraders of MDM2 Protein and Peptidomimetic Inhibitors Targeting WDR5-MLL1 Protein-Protein Interaction.
[4] Viktor Arnhold, et al. Reactivating TP53 signaling by the novel MDM2 inhibitor DS-3032b as a therapeutic option for high-risk neuroblastoma. ncotarget. 2018 Jan 5; 9(2): 2304–2319. DOI:10.18632/oncotarget.23409

Milademetan Preparation Products And Raw materials

Raw materials

Preparation Products

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Milademetan Suppliers

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1398568-47-2, MilademetanRelated Search:

Milademetan

DS-3032

L-erythro-Hexonamide, 2,6-anhydro-5-[[[(3'R,4'S,5'R)-6''-chloro-4'-(2-chloro-3-fluoro-4-pyridinyl)-1'',2''-dihydro-4,4-dimethyl-2''-oxodispiro[cyclohexane-1,2'-pyrrolidine-3',3''-[3H]indol]-5'-yl]carbonyl]amino]-3,4,5-trideoxy-

DS-3032B (Milademetan)

Milademetan (DS-3032)

DS-3032 (MILADEMETAN) (DS-3032B)

(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

Milademetan, 10 mM in DMSO

1398568-47-2

C30H34Cl2FN5O4