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ERK-IN-3

  Cat. No.:  DC42417   Featured
Chemical Structure
2055597-12-9
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More than 5000 active chemicals with high quality for research!
Field of application
ERK-IN-3 is a potent and oral of ERK. ERK-IN-3 inhibits ERK1/2 with low single-digit nM IC50 values. ERK-IN-3 has the potential to be used to study cancers driven by RAS mutations.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 2055597-12-9
Chemical Name: Erk-IN-3
Synonyms: ERK-IN-3;ASN007;NSC828319;NC[C@H](C1=CC(=CC(=C1)F)Cl)NC(=O)C=1N=CN(C=1)C1=NC(=NC=C1C)NC1CCOCC1
SMILES: ClC1=CC(=CC(=C1)[C@@H](CN)NC(C1=CN(C=N1)C1=C(C)C=NC(=N1)NC1CCOCC1)=O)F
Formula: C22H25ClFN7O2
M.Wt: 473.931006193161
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: ERK-IN-3 is a potent and oral of ERK. ERK-IN-3 inhibits ERK1/2 with low single-digit nM IC50 values. ERK-IN-3 has the potential to be used to study cancers driven by RAS mutations.
Target: ERK1 ERK2
In Vivo: 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 Vitro: 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].
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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Cat. No. Product name Field of application
DC42417 ERK-IN-3 ERK-IN-3 is a potent and oral of ERK. ERK-IN-3 inhibits ERK1/2 with low single-digit nM IC50 values. ERK-IN-3 has the potential to be used to study cancers driven by RAS mutations.
DC40360 ERK1/2 inhibitor 2(ASTX-029) ERK1/2 inhibitor 2 (Example 1) is a potent dual ERK1/2 inhibitor. ERK1/2 inhibitor 2 has anti-cancer activity.
DC10640 LY3214996 LY3214996 is a selective and novel ERK1/2 inhibitor with IC50 of 5 nM for both enzymes in biochemical assays. It potently inhibits cellular phospho-RSK1 in BRAF and RAS mutant cancer cell lines.
DC11481 AZD-0364 AZD-0364 is a potent and selective ERK2 inhibitor extracted from patent WO2017080979A1, compound example 18, has an IC50 of 0.6 nM.
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