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. MS 154 decreases EGFR protein levels, inhibits downstream signaling in and inhibits proliferation of mutant EGFR-bearing lung cancer cells (DC50 values 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. It is bioavailable in mice following ip administration.
MedKoo Cat#: 533717
Name: MS154
CAS#: 2550393-21-8
Chemical Formula: C46H54ClFN8O8
Exact Mass: 900.3737
Molecular Weight: 901.43
Elemental Analysis: C, 61.29; H, 6.04; Cl, 3.93; F, 2.11; N, 12.43; O, 14.20
| Solvent | mg/mL | mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 90.1 | 100.00 |
The following data is based on the product molecular weight 901.43 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 |
