1H-Imidazole-4-carboxamide, N-[(1S)-2-amino-1-(3-chloro-5-fluorophenyl)ethyl]-1-[5-methyl-2-[(tetrahydro-2H-pyran-4-yl)amino]-4-pyrimidinyl]-, compd. with benzenesulfonate (1:1)
- CAS No.
- 2055597-39-0
- Chemical Name:
- 1H-Imidazole-4-carboxamide, N-[(1S)-2-amino-1-(3-chloro-5-fluorophenyl)ethyl]-1-[5-methyl-2-[(tetrahydro-2H-pyran-4-yl)amino]-4-pyrimidinyl]-, compd. with benzenesulfonate (1:1)
- Synonyms
- ASN007 benzenesulfonate;ERK-IN-3 benzenesulfonate;1H-Imidazole-4-carboxamide, N-[(1S)-2-amino-1-(3-chloro-5-fluorophenyl)ethyl]-1-[5-methyl-2-[(tetrahydro-2H-pyran-4-yl)amino]-4-pyrimidinyl]-, compd. with benzenesulfonate (1:1)
- CBNumber:
- CB49858293
- Molecular Formula:
- C28H31ClFN7O5S
- Molecular Weight:
- 632.11
- MDL Number:
- MOL File:
- 2055597-39-0.mol
1H-Imidazole-4-carboxamide, N-[(1S)-2-amino-1-(3-chloro-5-fluorophenyl)ethyl]-1-[5-methyl-2-[(tetrahydro-2H-pyran-4-yl)amino]-4-pyrimidinyl]-, compd. with benzenesulfonate (1:1) Chemical Properties,Uses,Production
Biological Activity
ERK-IN-3 benzenesulfonate is a potent and orally active inhibitor of ERK. ERK-IN-3 benzenesulfonate inhibits ERK1/2 with low single-digit nM IC50 values. ERK-IN-3 benzenesulfonate can be used for the research of cancers driven by RAS mutations[1]. ERK-IN-3 inhibits the phosphorylation of ERK1/2 substrates such as RSK1, FRA1, and Elk1 in various cell lines[1].ERK-IN-3 showes single-digit nanomolar antiproliferative activity that is selective for MAPK-pathway dependent cancer cell lines[1]. ERK-IN-3 (daily p.o.) inhibits tumor growth in multiple BRAF and KRAS mutant xenograft models in mice and was well tolerated at efficacious doses[1].
References
[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).
1H-Imidazole-4-carboxamide, N-[(1S)-2-amino-1-(3-chloro-5-fluorophenyl)ethyl]-1-[5-methyl-2-[(tetrahydro-2H-pyran-4-yl)amino]-4-pyrimidinyl]-, compd. with benzenesulfonate (1:1) Preparation Products And Raw materials
Raw materials
Preparation Products
1H-Imidazole-4-carboxamide, N-[(1S)-2-amino-1-(3-chloro-5-fluorophenyl)ethyl]-1-[5-methyl-2-[(tetrahydro-2H-pyran-4-yl)amino]-4-pyrimidinyl]-, compd. with benzenesulfonate (1:1) Suppliers
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
Aladdin Scientific | +1-833-552-7181 | sales@aladdinsci.com | United States | 52927 | 58 |
TargetMol Chemicals Inc. | 15002134094 | marketing@targetmol.com | China | 24246 | 58 |
Supplier | Advantage |
---|---|
Aladdin Scientific | 58 |
TargetMol Chemicals Inc. | 58 |