SCH772984

Bezeichnung:SCH772984

CAS-Nr942183-80-4

Englisch Name:SCH772984

CBNumberCB12473742

SummenformelC33H33N9O2

Molgewicht587.67

MOL-Datei942183-80-4.mol

SCH772984 physikalisch-chemischer Eigenschaften

Schmelzpunkt	>214°C (dec.)
Siedepunkt	857.3±65.0 °C(Predicted)
Dichte	1.353±0.06(20.0000℃)
storage temp.	Refrigerator
Löslichkeit	DMSO (Slightly)
pka	12.05±0.40(Predicted)
Aggregatzustand	Solid
Farbe	Pale Yellow
CAS Datenbank	942183-80-4

Sicherheit

HS Code

29339900

Gefahreninformationscode (GHS)

SCH772984 Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
The 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.
Verwenden
SCH772984 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.
Definition
ChEBI: 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.
target
ERK1

SCH772984 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

942183-80-4, SCH772984 Verwandte Suche:

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