MS39 is a novel E3 ligase von Hippel-Lindau-recruiting EGFR degrader. MS 39 potently induces degradation of mutant EGFR (DC50 values are 5 nM and 3.3 nM in HCC827 (exon 19 del) and H3255 (L858R mutation) lung cancer cell lines, respectively), but exhibits no significant effect in cell lines bearing wild-type EGFR at concentrations up to 10 μM. MS 39 inhibits proliferation of H3255 lung cancer cells in vitro, and is bioavailable in mice following ip administration.
MedKoo Cat#: 533718
Name: MS39
CAS#: 2675490-92-1
Chemical Formula: C55H71ClFN9O7S
Exact Mass: 1055.4870
Molecular Weight: 1056.74
Elemental Analysis: C, 62.51; H, 6.77; Cl, 3.35; F, 1.80; N, 11.93; O, 10.60; S, 3.03
| Solvent | mg/mL | mM | |
|---|---|---|---|
| Solubility | |||
| Soluble in DMSO | 0.0 | 100.00 |
The following data is based on the product molecular weight 1,056.74 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 |
