MD-224

• Description:

  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 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

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category:

  Reference compound1

• Clinical Information:

  No Development Reported

• Isoform:

  MDM2

• CAS Number:

  2136247-12-4