| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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Milademetan tosylate hydrate (also called DS3032b; DS-3032), the tosylate salt and hydrated form of Milademetan, is a potent, selective and orally bioactive MDM2 inhibitor with potential antitumor activity.
| ln Vitro |
In wild-type TP53 neuroblastoma cells, meledemetan (DS-3032) preferentially promotes the expression of CDKNA1, BAX, and MDM2 while stabilizing TP53 [3]. Treatment with meledemetan (DS-3032b) increases the expression of the TP53 target gene and causes apoptosis, senescence, and G1 cell cycle arrest [3]. Regardless of MYCN status, treatment with meledemetan (DS-3032b, 0-2000 nM) specifically decreases the viability, proliferation, and migration of neuroblastoma cells carrying wild-type TP53 [4].
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|---|---|
| ln Vivo |
Milademetan (DS-3032b, 50 mg/kg, orally administered) xenografts neuroblastoma cells with functioning TP53, delaying tumor growth and enhancing survival [4].
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| Cell Assay |
Cell viability assay[4]
Cell Types: SK-N-SH, SH-SY5Y, IMR32, IMR5 and LAN5 cell lines. Tested Concentrations: 0-2000 nM. Incubation Duration: 24-72 hrs (hours). Experimental Results: Vitality diminished in a dose- and time-dependent manner. In SK-N-SH, SH-SY5Y, IMR32, IMR5 and LAN5 cell lines (72 hrs (hours)), the IC50 values were 21.9 nM, 17.7 nM, 52.63 nM, 25.7 nM and 44.1 nM, respectively. |
| Animal Protocol |
Animal/Disease Models: SH-SY5Y nude mouse xenograft tumor [4].
Doses: 50 mg/kg. Dosing: po (oral gavage) for 30 days, alternating with 4 days of po (oral gavage) treatment and then 2 days of no treatment (4+2). Experimental Results: The survival rate of the mouse group was Dramatically prolonged. diminished neuroblastoma xenograft tumor growth through activation of TP53 signaling. |
| References |
| Molecular Formula |
C₃₇H₄₄CL₂FN₅O₈S
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|---|---|
| Molecular Weight |
808.74
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| Exact Mass |
807.227
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| CAS # |
2095625-97-9
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| Related CAS # |
Milademetan;1398568-47-2
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| PubChem CID |
89051550
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
54
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| Complexity |
1290
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| Defined Atom Stereocenter Count |
5
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| SMILES |
CC1=CC=C(C=C1)S(=O)(=O)O.CC1(CCC2(CC1)[C@@]3([C@H]([C@@H](N2)C(=O)N[C@@H]4CC[C@H](OC4)C(=O)N)C5=C(C(=NC=C5)Cl)F)C6=C(C=C(C=C6)Cl)NC3=O)C.O
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| InChi Key |
WPJOGWGXMTUHPW-CIPNXXNHSA-N
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| InChi Code |
InChI=1S/C30H34Cl2FN5O4.C7H8O3S.H2O/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);1H2/t16-,20+,21+,23-,30-;;/m1../s1
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| Synonyms |
DS3032b tosylate hydrate DS-3032b DS-3032DS 3032b DS 3032DS3032 DS-3032b tosylate Milademetan tosylate hydrate
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~61.82 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 5 mg/mL (6.18 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 5 mg/mL (6.18 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 5 mg/mL (6.18 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.2365 mL | 6.1825 mL | 12.3649 mL | |
| 5 mM | 0.2473 mL | 1.2365 mL | 2.4730 mL | |
| 10 mM | 0.1236 mL | 0.6182 mL | 1.2365 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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