For research use only. Not for therapeutic Use.
ASN007 (ERK-IN-3) benzenesulfonate is a potent and orally active inhibitor of ERK. ASN007 benzenesulfonate inhibits ERK1/2 with low single-digit nM IC50 values. ASN007 benzenesulfonate can be used for the research of cancers driven by RAS mutations[1].
ASN007 inhibits the phosphorylation of ERK1/2 substrates such as RSK1, FRA1, and Elk1 in various cell lines[1].
ASN007 showes single-digit nanomolar antiproliferative activity that is selective for MAPK-pathway dependent cancer cell lines[1].
ASN007 (daily p.o.) inhibits tumor growth in multiple BRAF and KRAS mutant xenograft models in mice and was well tolerated at efficacious doses[1].
| Catalog Number | I044492 |
| CAS Number | 2055597-39-0 |
| Synonyms | N-[(1S)-2-amino-1-(3-chloro-5-fluorophenyl)ethyl]-1-[5-methyl-2-(oxan-4-ylamino)pyrimidin-4-yl]imidazole-4-carboxamide;benzenesulfonic acid |
| Molecular Formula | C28H31ClFN7O5S |
| Purity | ≥95% |
| InChI | InChI=1S/C22H25ClFN7O2.C6H6O3S/c1-13-10-26-22(28-17-2-4-33-5-3-17)30-20(13)31-11-19(27-12-31)21(32)29-18(9-25)14-6-15(23)8-16(24)7-14;7-10(8,9)6-4-2-1-3-5-6/h6-8,10-12,17-18H,2-5,9,25H2,1H3,(H,29,32)(H,26,28,30);1-5H,(H,7,8,9)/t18-;/m1./s1 |
| InChIKey | JXWBNMQMMAONIH-GMUIIQOCSA-N |
| SMILES | CC1=CN=C(N=C1N2C=C(N=C2)C(=O)NC(CN)C3=CC(=CC(=C3)Cl)F)NC4CCOCC4.C1=CC=C(C=C1)S(=O)(=O)O |
| Reference | [1]. Sanjeeva PR, et, al. Abstract B150: ASN007, a novel oral ERK inhibitor, shows robust antitumor activity in RAS mutant cancer models. Molecular Cancer Therapeutics. 2018 Jan; 17(1). |
