[CAS NO. 2136246-72-3] MD-222
PRODUCTS SPECIFICATIONS [2136246-72-3]
DESCRIPTION [2136246-72-3]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 893.83 |
| Molecular Formula | C48H47Cl2FN6O6 |
| SMILES | O=C1[C@]2(C3=CC=C(Cl)C=C3N1)C4(CCCCC4)N[C@H]([C@]2([H])C5=C(C(Cl)=CC=C5)F)C(NC6=CC=C(C=C6)C(NCCCCCC7=C8C(C(N(C9C(NC(CC9)=O)=O)C8)=O)=CC=C7)=O)=O |
Summary
IC50 & Target
|
MDM2 |
In Vitro
MD-222 (1-30 nM; 1-2 hours) treatment shows very effective in reducing the levels of MDM2 protein and increasing the levels of p53 in a time- and dose-dependent manner in RS4;11 and RS4;11/IRMI-2 cells
[1]
.
MD-222 (30-100 nM; 6 hours) is effective in increasing the expression of several p53-targeted genes, such as MDM2, CDKN1A, and PUMA in RS4;11 cells, indicating strong activation of p53
[2]
.
MD-222 (4 days) shows cell growth inhibitory activity in RS4;11 cells with an IC50 of 5.5 nM, and has no effect on RS4;11/IRMI-2, MDA-MB-231 and MDA-MB-468 cells
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Western Blot Analysis [1]
| Cell Line: | RS4;11 and RS4;11/IRMI-2 cells |
| Concentration: | 1 nM, 3 nM, 10 nM, 30 nM |
| Incubation Time: | 1 hour, 2 hours |
| Result: | Reduced the level of MDM2 and increased the level of p53. |
RT-PCR [2]
| Cell Line: | RS4;11 cells |
| Concentration: | 30 nM, 100 nM |
| Incubation Time: | 6 hours |
| Result: | Increasd the expression of several p53-targeted genes, such as MDM2, CDKN1A, and PUMA. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 200 mg/mL ( 223.76 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 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 |
-
1.
-
2.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 5 mg/mL (5.59 mM); Clear solution
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.