SCH772984 hydrochloride
- Parent CAS: 942183-80-4
- Optical Purity: 99% e.e.
- Soluble in 0.1N HCl(aq) and DMSO
- MF: C33H33N9O2.HCl
- MW: 624.14
Description
Extracellular signal regulated kinase (ERK) is a pivotal enzyme in the pathway downstream of Ras, Raf, and MEK, acting as a central link between multiple signaling pathways. SCH772984 is a potent, specific and ATP competitive inhibitor of ERK1 and ERK2 with IC50s at low nMs. It inhibits phosphorylation of the ERK substrate p90 ribosomal S6 kinase (T359/S363 phospho-RSK) in a dose-dependent manner, and also inhibits phosphorylation of residues in the activation loop of ERK itself. More importantly, it effectively inhibits MAPK signaling and cell proliferation in BRAF or MEK inhibitor-resistant models as well as in tumor cells resistant to concurrent treatment with BRAF and MEK inhibitors.
More Information
| Parent CAS No. | 942183-80-4 |
|---|---|
| Chemical Name | (R)-1-(2-oxo-2-(4-(4-(pyrimidin-2-yl)phenyl)piperazin-1-yl)ethyl)-N-(3-(pyridin-4-yl)-1H-indazol-5-yl)pyrrolidine-3-carboxamide hydrochloride |
| extra_info | Sold in collaboration with Chemietek |
| SMILES | C12NN=C(C3C=CN=CC=3)C1=CC(NC([C@@H]1CCN(C1)CC(=O)N1CCN(CC1)C1C=CC(=CC=1)C1=NC=CC=N1)=O)=CC=2.Cl |&1:15,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C33H33N9O2.ClH/c43-30(42-18-16-41(17-19-42)27-5-2-24(3-6-27)32-35-11-1-12-36-32)22-40-15-10-25(21-40)33(44)37-26-4-7-29-28(20-26)31(39-38-29)23-8-13-34-14-9-23;/h1-9,11-14,20,25H,10,15-19,21-22H2,(H,37,44)(H,38,39);1H/t25-;/m1./s1 |
| InChiKey | QBCBHOVUUGUMBJ-VQIWEWKSSA-N |
| CID | 146035694 |
| Short Description | ERK1 and ERK2 inhibitor |
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