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
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
N-Bromosuccinimide Price
- Product number
- CS-0021065
- Product name
- Milademetan
- Purity
- 98.16%
- Packaging
- 1mg
- Price
- $220
- Updated
- 2021/12/16
- Product number
- CS-0021065
- Product name
- Milademetan
- Purity
- 98.16%
- Packaging
- 5mg
- Price
- $660
- Updated
- 2021/12/16
- Product number
- CS-0021065
- Product name
- Milademetan
- Purity
- 98.16%
- Packaging
- 10mg
- Price
- $1100
- Updated
- 2021/12/16
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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