MD-224

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 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.

Product Specifications

CAS Number

[2136247-12-4]

Product Name Alternative

trans-1-Aminocyclobutane-1,3-dicarboxylic acid,R80130,(S)-4-Carboxyphenylglycine,cis-1-Aminocyclobutane-1,3-dicarboxylic acid

UNSPSC

12352005

Hazard Statement

H315, H319, H320

Target

E1/E2/E3 Enzyme; MDM-2/p53; PROTACs

Type

Reference compound

Related Pathways

Apoptosis; Metabolic Enzyme/Protease; PROTAC

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/md-224.html

Purity

99.60

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

FC1=C(Cl)C=CC=C1[C@@H]2[C@@]3(C(C=CC(Cl)=C4)=C4NC3=O)C5(CCCCC5)N[C@H]2C(NC6=CC=C(C(NCCCC#CC7=C(CN(C8C(NC(CC8)=O)=O)C9=O)C9=CC=C7)=O)C=C6)=O

Molecular Formula

C48H43Cl2FN6O6

Molecular Weight

889.80

Precautions

H315, H319, H320

References & Citations

[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