Identification | Back Directory | [Name]
ASN007 | [CAS]
2055597-12-9 | [Synonyms]
ASN007 ERK-IN-3 ASN007(ERAS 007) ASN007 free base N-[(1S)-2-amino-1-(3-chloro-5-fluorophenyl)ethyl]-1-{5-methyl-2-[(oxan-4-yl)amino]pyrimidin-4-yl}-1H-imidazole-4-carboxamide | [Molecular Formula]
C22H25ClFN7O2 | [MOL File]
2055597-12-9.mol | [Molecular Weight]
473.93 |
Chemical Properties | Back Directory | [density ]
1.48±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 250 mg/mL (527.50 mM; Need ultrasonic) | [form ]
Solid | [pka]
12.73±0.46(Predicted) | [color ]
White to light yellow |
Hazard Information | Back Directory | [Biological Activity]
ERK-IN-3 is a potent and orally active inhibitor of ERK. ERK-IN-3 inhibits ERK1/2 with low single-digit nM IC50 values. ERK-IN-3 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]. | [storage]
Store at -20°C | [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). |
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