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Chemical Structure| 2136247-12-4 Chemical Structure| 2136247-12-4

Structure of MD-224
CAS No.: 2136247-12-4

Chemical Structure| 2136247-12-4

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MD-224 is a potent small-molecule degrader of mouse double minute 2 homolog (MDM2) based on the proteolysis-targeting chimera (PROTAC) technology. MD-224 induced rapid degradation of MDM2 (<1 nM) and inhibited RS4 in human leukemia cells. The IC50 value of cell growth was 1.5 nM.

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Product Details of MD-224

CAS No. :2136247-12-4
Formula : C48H43Cl2FN6O6
M.W : 889.80
SMILES Code : O=C([C@H](N1)[C@H](C2=CC=CC(Cl)=C2F)[C@]3(C(NC4=C3C=CC(Cl)=C4)=O)C51CCCCC5)NC6=CC=C(C(NCCCC#CC7=CC=CC8=C7CN(C(CC9)C(NC9=O)=O)C8=O)=O)C=C6
MDL No. :MFCD32201043

Safety of MD-224

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
NTERA-2 cells 10 µM 24 hours Evaluate the degradation ability of 6-fluoro lenalidomide on SALL4 Nat Commun. 2023 Aug 18;14(1):4683
HuH7 cells 10 µM 24 hours Evaluate the degradation ability of 6-fluoro lenalidomide on SALL4 and PLZF Nat Commun. 2023 Aug 18;14(1):4683
MM1.S cells 10 µM 24 hours Evaluate the degradation ability of 6-fluoro lenalidomide on IKZF1, IKZF3, and CK1α Nat Commun. 2023 Aug 18;14(1):4683
MV4;11 cells <1 nM 2 hours Induces MDM2 protein degradation and p53 protein accumulation, inhibits cell growth J Med Chem. 2019 Jan 24;62(2):448-466
RS4;11 cells <1 nM 2 hours Induces MDM2 protein degradation and p53 protein accumulation, inhibits cell growth with IC50 value of 1.5 nM J Med Chem. 2019 Jan 24;62(2):448-466

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice RS4;11 xenograft tumor model Intravenous 25 mg/kg Weekly for 2 weeks Achieves complete and durable tumor regression J Med Chem. 2019 Jan 24;62(2):448-466

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.12mL

0.22mL

0.11mL

5.62mL

1.12mL

0.56mL

11.24mL

2.25mL

1.12mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2
 

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