| Identification | Back Directory | [Name]
MD-224 | [CAS]
2136247-12-4 | [Synonyms]
MD-224
11,E1/E2/E3 Enzyme,leukemia,PROTACs,E2 conjugating enzyme,MD 224
MD224,inhibit,PROTAC,Ubiquitin activating enzyme,Ubiquitin ligase,Inhibitor,MDM-2/p53,cancer,MD-224,E1 activating enzyme,Ubiquitin conjugating enzyme,E3 ligating enzyme,RS4
Dispiro[cyclohexane-1,2'-pyrrolidine-3',3''-[3H]indole]-5'-carboxamide, 6''-chloro-4'-(3-chloro-2-fluorophenyl)-N-[4-[[[5-[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1-oxo-1H-isoindol-4-yl]-4-pentyn-1-yl]amino]carbonyl]phenyl]-1'',2''-dihydro-2''-oxo-, (3'R,4'S,5'R)- | [Molecular Formula]
C48H43Cl2FN6O6 | [MDL Number]
MFCD32201043 | [MOL File]
2136247-12-4.mol | [Molecular Weight]
889.81 |
| Chemical Properties | Back Directory | [density ]
1.49±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO:100.0(Max Conc. mg/mL);112.38(Max Conc. mM) | [form ]
Solid | [pka]
10.67±0.40(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
MD-224 is a first-in-class and highly potent small-molecule human murine double minute 2 (MDM2) degrader based on the proteolysistargeting chimera (PROTAC) concept. MD-224 consists of ligands for Cereblon and MDM2. MD-224 induces rapid degradation of MDM2 at concentrations <1 nM in human leukemia cells, and achieves an IC50 value of 1.5 nM in inhibition of growth of RS4;11 cells. MD-224 has the potential to be a new class of anticancer agent[1]. MD-224 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. | [IC 50]
MDM2: 1 nM (IC50) | [storage]
Store at -20°C | [References]
[1] 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 DOI:10.1021/acs.jmedchem.8b00909 |
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