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Supplier NameMedChemExpress (MCE)
Contactsales
Tel609-228-6898
Mobile609-228-6898
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Emailsales@medchemexpress.com; tech@medchemexpress.com
Websitehttp://www.medchemexpress.com/
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Product NameSCH772984
SynonymsSCH772984
(R)-1-(2-oxo-2-(4-(4-(pyrimidin-2-yl)phenyl)piperazin-1-yl)ethyl)-N-(3-(pyridin-4-yl)-1H-indazol-5-
(3R)-1-[2-Oxo-2-[4-[4-(2-pyrimidinyl)phenyl]-1-piperazinyl]ethyl]-N-[3-(4-pyridinyl)-1H-indazol-5-yl]-3-pyrrolidinecarboxamide

Synonyms

SCH772984
(R)-1-(2-oxo-2-(4-(4-(pyrimidin-2-yl)phenyl)piperazin-1-yl)ethyl)-N-(3-(pyridin-4-yl)-1H-indazol-5-
(3R)-1-[2-Oxo-2-[4-[4-(2-pyrimidinyl)phenyl]-1-piperazinyl]ethyl]-N-[3-(4-pyridinyl)-1H-indazol-5-yl]-3-pyrrolidinecarboxamide
(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
(3R)-1-[2-Oxo-2-[4-[4-(2-pyrimidinyl)phenyl]-1-piperazinyl]ethyl]-N-[3-(4-pyridinyl)-1H-indazol-5-yl]-3-pyrrolidinecarboxamide SCH772984
CAS942183-80-4
EINECS1592732-453-0
Chemical FormulaC33H33N9O2
Molecular Weight587.67
inchi
Package10 mM * 1 mL;1 mg;2 mg;5 mg;10 mg;25 mg;50 mg
PriceEmail to quote
DescriptionsSCH772984

SCH772984

MedChemExpress (MCE)

HY-50846

942183-80-4

99.45%

Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months

Room temperature in continental US

Descriptions

SCH772984

SCH772984

MedChemExpress (MCE)

HY-50846

942183-80-4

99.45%

Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months

Room temperature in continental US
may vary elsewhere.

SCH772984 is a highly selective and ATP-competitive ERK inhibitor, with IC50s of 4 and 1 nM for ERK1 and ERK2, respectively. SCH772984 has antitumor activity in MAPK inhibitor-na?ve and MAPK inhibitor-resistant cells containing BRAF or RAS mutations.

SCH772984 (300 nM
24-48hours) results in a G1 arrest in SCH772984-sensitive melanoma cells[1]. SCH772984 (3-300 nM
24 hours) inhibits ERK and RSK phosphorylation[1]. SCH772984 shows EC50 values less than 500 nM in approximately 88% and 49% of BRAF-mutant (n=25) or RAS-mutant (n=35) tumor lines, respectively[1].

SCH772984 (12.5-50 mg/kg
i.p.
twice daily for 14 days) leads to 98% tumor regression[1]. Dose-dependent antitumor activity is also observed in the KRAS-mutant pancreatic MiaPaCa model, with 36% regression at 50 mg/kg twice daily. Importantly, tumor regression is accompanied by robust inhibition of ERK phosphorylation in tumor tissue. SCH772984 is well tolerated on this schedule as measured by morbidity, lethality, or body weight loss[1].

ERK2 1 nM (IC50) ERK1 4 nM (IC50)

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[1]. Morris EJ, et al. Discovery of a novel ERK inhibitor with activity in models of acquired resistance to BRAF and MEK inhibitors. Cancer Discov. 2013 Jul
3(7):742-50.
[Content Brief]

Supplier Websitehttp://www.medchemexpress.com/SCH772984.html
Last Update2025-10-14 16:03:33
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