| Size | Price | |
|---|---|---|
| 1mg | ||
| 5mg | ||
| 10mg | ||
| Other Sizes |
| Targets |
MDM2
|
|---|---|
| ln Vitro |
In RS4;11 and RS4;11/IRMI -2 cells, MD-222 (1-30 nM; 1-2 hours) treatment is particularly effective in lowering MDM2 protein levels and raising p53 levels in a time- and dose-dependent manner[1]. In RS4;11 cells, MD-222 (30-100 nM; 6 hours) is effective in upregulating the expression of multiple p53-targeted genes, including MDM2, CDKN1A, and PUMA, demonstrating robust p53 activation[2]. MD-222 (4 days) had no effect on RS4;11/IRMI-2, MDA-MB-231, or MDA-MB-468 cells, but has cell growth inhibitory activity in RS4;11 cells with an IC50 of 5.5 nM[1].
|
| Cell Assay |
Western Blot Analysis[1]
Cell Types: RS4;11 and RS4;11/IRMI- 2 cells Tested Concentrations: 1 nM, 3 nM, 10 nM, 30 nM Incubation Duration: 1 hour, 2 hrs (hours) Experimental Results: decreased the level of MDM2 and increased the level of p53. RT-PCR[2] Cell Types: RS4;11 cells Tested Concentrations: 30 nM, 100 nM Incubation Duration: 6 hrs (hours) Experimental Results: Increased the expression of several p53-targeted genes, such as MDM2, CDKN1A, and PUMA. |
| References |
[1]. Jiuling Yang, et al. Simple Structural Modifications Converting a Bona fide MDM2 PROTAC Degrader into a Molecular Glue Molecule: A Cautionary Tale in the Design of PROTAC Degraders. J Med Chem. 2019 Nov 14;62(21):9471-9487.
[2]. Li Y, et al. Discovery of MD-224 as a First-in-Class, Highly Potent, and Efficacious Proteolysis TargetingChimera Murine Double Minute 2 Degrader Capable of Achieving Complete and Durable TumorRegression. J Med Chem. 2019 Jan 24;62(2):448-466. |
| Molecular Formula |
C48H47CL2FN6O6
|
|---|---|
| Molecular Weight |
893.83
|
| CAS # |
2136246-72-3
|
| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
|
| SMILES |
O=C1CCC(N2CC3C(CCCCCNC(C4=CC=C(NC(=O)[C@H]5[C@H](C6=C(C(Cl)=CC=C6)F)[C@@]6(C7C(=CC(Cl)=CC=7)NC6=O)C6(CCCCC6)N5)C=C4)=O)=CC=CC=3C2=O)C(=O)N1
|
| HS Tariff Code |
2934.99.9001
|
| 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, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : 200 mg/mL (223.76 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 5 mg/mL (5.59 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 (5.59 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. 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 corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.1188 mL | 5.5939 mL | 11.1878 mL | |
| 5 mM | 0.2238 mL | 1.1188 mL | 2.2376 mL | |
| 10 mM | 0.1119 mL | 0.5594 mL | 1.1188 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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