ASN007, a novel oral ERK inhibitor, shows robust antitumor activity in RAS mutant cancer models. with low single-digit nM IC50 values. ASN007 showed a slow dissociation rate (long target residence time) as compared to several other known ERK inhibitors. In mechanistic cell-based assays, ASN007 inhibited the phosphorylation of ERK1/2 substrates such as RSK1, FRA1, and Elk1 in various cell lines. ASN007 showed single-digit nanomolar antiproliferative activity that was selective for MAPK-pathway dependent cancer cell lines.
MedKoo Cat#: 207046
Name: ASN007 free base
CAS#: 2055597-12-9 (free base)
Chemical Formula: C22H25ClFN7O2
Exact Mass: 473.1742
Molecular Weight: 473.94
Elemental Analysis: C, 55.75; H, 5.32; Cl, 7.48; F, 4.01; N, 20.69; O, 6.75
Solvent | mg/mL | mM | |
---|---|---|---|
Solubility | |||
DMSO | 200.0 | 421.99 |
The following data is based on the product molecular weight 473.94 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 |