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| 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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| MSDS_26024_DC42417_2055597-12-9 |
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