MD-4251 is a First-in-Class Oral MDM2 Degrader Inducing Complete Tumor Regression with Single-Dose Administration. MD-4251 inducespotent and rapid MDM2 degradation in RS4;11 cells (DC50 = 0.2 nM; Dmax = 96% at 2 h), leading to robust p53 activation. Itselectively inhibits the growth of acute leukemia cell lines with wild-type p53, with minimal activity in p53 mutant lines. MD-4251shows excellent oral bioavailability in mice, favorable metabolic stability, and no CYP or hERG liabilities. A single oral dose inducessustained MDM2 depletion and attains complete tumor regression in vivo.
MedKoo Cat#: 129053
Name: MD-4251
CAS#: N/A
Chemical Formula: C47H53Cl2FN8O4
Exact Mass: 882.3600
Molecular Weight: 883.89
Elemental Analysis: C, 63.87; H, 6.04; Cl, 8.02; F, 2.15; N, 12.68; O, 7.24
The following data is based on the product molecular weight 883.89 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
Acharyya RK, Huang L, Aguilar A, Hu B, Bai L, Metwally H, McEachern D, Jiang W, Wang Y, Li Q, Wen B, Sun D, Wang S. MD-4251: A First-in-Class Oral MDM2 Degrader Inducing Complete Tumor Regression with Single-Dose Administration. J Med Chem. 2025 Jun 13. doi: 10.1021/acs.jmedchem.5c00809. Epub ahead of print. PMID: 40511819.
