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2055597-12-9

2055597-12-9 Structure

2055597-12-9 Structure
IdentificationBack 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 PropertiesBack 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 InformationBack Directory
[Uses]

ASN007 (ERK-IN-3) is a potent and orally active inhibitor of ERK. ASN007 inhibits ERK1/2 with low single-digit nM IC50 values. ASN007 can be used for the research of cancers driven by RAS mutations[1].
[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].
[in vivo]

ASN007 (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].

[IC 50]

ERK1; ERK2
[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).
Spectrum DetailBack Directory
[Spectrum Detail]

ASN007(2055597-12-9)1HNMR
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