SCH772984

SCH772984 Basic information
Product Name:SCH772984
Synonyms:SCH772984;SCH772984/SCH-772984;(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;(R)-1-(2-oxo-2-(4-(4-(pyrimidin-2-yl)phenyl)piperazin-1-yl)ethyl)-N-(3-(pyridin-4-yl)-1H-indazol-5-;SCH772984, >=98%;(3R)-1-[2-Oxo-2-[4-[4-(2-pyrimidinyl)phenyl]-1-piperazinyl]ethyl]-N-[3-(4-pyridinyl)-1H-indazol-5-yl]-3-pyrrolidinecarboxamide, 98%, a selective inhibitor of ERK1/2
CAS:942183-80-4
MF:C33H33N9O2
MW:587.67
EINECS:1592732-453-0
Product Categories:Inhibitors;api;MAPK
Mol File:942183-80-4.mol
SCH772984 Structure
SCH772984 Chemical Properties
Melting point >214°C (dec.)
Boiling point 857.3±65.0 °C(Predicted)
density 1.353±0.06(20.0000℃)
storage temp. Refrigerator
solubility DMSO (Slightly)
pka12.05±0.40(Predicted)
form Solid
color Pale Yellow
CAS DataBase Reference942183-80-4
Safety Information
HS Code 29339900
MSDS Information
SCH772984 Usage And Synthesis
DescriptionThe extracellular regulated kinases 1 and 2 (ERK1/2) are functionally redundant kinases activated by a variety of growth factors and mitogens. SCH 772984 is a potent inhibitor of ERK1 and ERK2 (IC50s = 4 and 1 nM, respectively). 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. 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.
UsesSCH772984 is a novel and selective inhibitor of ERK1/2 that displays behaviors of both type I and type II kinase inhibitors and has nanomolar cellular potency in tumor cells with mutations in BRAF, NRA5, or KRAS and induces tumor regressions in xenograft models.
DefinitionChEBI: SCH772984 is a member of the class of indazoles that is 1H-indazole substituted by pyridin-4-yl and {[(3R)-1-(2-oxo-2-{4-[4-(pyrimidin-2-yl)phenyl]piperazin-1-yl}ethyl)pyrrolidin-3-yl]carbonyl}amino groups at positions 3 and 5, respectively. It is a potent inhibitor of mitogen-activated protein kinases ERK1 and ERK2 (IC50 = 4 and 1 nM, respectively) that exhibits anti-cancer properties. It has a role as an antineoplastic agent, an EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor, an apoptosis inducer and an analgesic. It is a member of pyridines, a biaryl, a secondary carboxamide, a pyrrolidinecarboxamide, a member of indazoles, a tertiary amino compound, a N-acylpiperazine, a N-arylpiperazine, a member of pyrimidines, a N-alkylpyrrolidine and a tertiary carboxamide.
targetERK1
SCH772984 Preparation Products And Raw materials
SB 203580 PD 0332991 HCl Trimethoprim 2-(2-FURANYL)-7-[3-(4-METHOXYPHENYL)PROPYL]-7H-PYRAZOLO[4,3-E][1,2,4]TRIAZOLO[1,5-C]PYRIMIDIN-5-AMINE Methylthiouracil Trametinib 6-(p-Nitrophenyl)pyrrolo[2,1-d][1,5]benzothiazepine 5,5-dioxide 7H-Pyrrolo[3,2-f]quinazoline-1,3-diaMine, N3-cyclopropyl-7-[[4-(1-Methylethyl)phenyl]Methyl]-, (Hydrochloride) (1:2) R-(-)-7-Chloro-8-hydroxy-3-methyl-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine, hydrochloride 1,9-Pyrazoloanthrone MK-2206 2HCl SCH54292 SCH 58261 Sulfamonomethoxine Propylthiouracil

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