MS 154

• Target:

  EGFR|||PROTACs|||Others

• Related Pathways:

  PROTAC|||JAK/STAT signaling|||Tyrosine Kinase/Adaptors|||Angiogenesis|||Others

• Bioactivity:

  MS 154 is a potent and selective cereblon-recruiting Degrader (PROTAC®) of mutant epidermal growth factor receptor (EGFR), comprising a cereblon-binding moiety joined by a linker to gefitinib (Iressa) . MS 154 decreases EGFR protein levels, inhibits downstream signaling in and inhibits proliferation of mutant EGFR-bearing lung cancer cells (DC50values are 11 and 25 nM in HCC-827 and H3255 cells, respectively; Dmax> 95% at 50 nM), but not in WT-EGFR-bearing ovarian and lung cancer cells lines. Bioavailable in mice following ip administration.

• Smiles:

  O=C1C=2C(C(=O)N1C3C(=O)NC(=O)CC3)=CC=CC2OCCCCCCCCNC(CCN4CCN(CCCOC5=CC6=C(C=C5OC)N=CN=C6NC7=CC(Cl)=C(F)C=C7)CC4)=O

• Molecular Formula:

  C46H54ClFN8O8

• Molecular Weight:

  901.42

• Shipping Conditions:

  Cool pack

• Storage Temperature:

  -20°C

• CAS Number:

  2550393-21-8