A potent

SCH 772984 – 5 mg

Brand:
Cayman
CAS:
942183-80-4
Storage:
-20
UN-No:
Non-Hazardous - /

The extracellular regulated kinases 1 and 2 (ERK1/2) are functionally redundant kinases activated by a variety of growth factors and mitogens.{17806} SCH 772984 is a potent inhibitor of ERK1 and ERK2 (IC50s = 4 and 1 nM, respectively).{30913} It is highly selective, with only seven kinases of 300 tested showing more than 50% inhibition at a concentration of 1 µM. SCH 772984 has nanomolar cytotoxicity in tumor cells with mutations in BRAF, NRAS, or KRAS.{30913} It is effective in vivo, inducing regression of xenograft tumors in mice. SCH 772984 displays slow binding kinetics, binding to a novel binding pocket in inactive ERK isoforms.{30912}  

 

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Description

A potent, selective inhibitor of ERK1 and ERK2 (IC50s = 4 and 1 nM, respectively); has nanomolar cytotoxicity in tumor cells with mutations in BRAF, NRAS, or KRAS; effective in vivo, inducing regression of xenograft tumors in mice

Formal name: (3R)-1-[2-oxo-2-[4-[4-(2-pyrimidinyl)phenyl]-1-piperazinyl]ethyl]-N-[3-(4-pyridinyl)-1H-indazol-5-yl]-3-pyrrolidinecarboxamide

Synonyms: 

Molecular weight: 587.7

CAS: 942183-80-4

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|RAS/RAF/MEK/ERK/MAPK||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Death||Research Area|Cancer|Cell Signaling|ERK/MAPK Signaling

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