Ulixertinib hydrochloride Struktur

Ulixertinib hydrochloride

Bezeichnung:Ulixertinib hydrochloride

CAS-Nr1956366-10-1

Englisch Name:Ulixertinib hydrochloride

CBNumberCB53133892

SummenformelC21H23Cl3N4O2

Molgewicht469.79192

MOL-Datei1956366-10-1.mol

Ulixertinib hydrochloride physikalisch-chemischer Eigenschaften

Schmelzpunkt	231-232°C
storage temp.	-20°C Freezer
Löslichkeit	DMSO (Slightly), Methanol (Slightly)
Aggregatzustand	Solid
Farbe	White to Off-White
InChIKey	DKGYQCPFBWFTHM-JHTMQSDJNA-N
SMILES	O=C(N[C@H](CO)C1C=C(Cl)C=CC=1)C1NC=C(C2C(Cl)=CN=C(NC(C)C)C=2)C=1.Cl \|&1:3,r\|

Sicherheit

HS Code

2933998090

Gefahreninformationscode (GHS)

Ulixertinib hydrochloride Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
Ulixertinib is a reversible ERK1/2 inhibitor that demonstrates an IC₅₀ value of <0.3 nM for ERK2. In A375 melanoma cells with b-Raf^V600E mutation, it has been reported to reduce the levels of phosphorylated ERK2 and the downstream kinase RSK (IC₅₀s = 4.1 and 0.14 μM, respectively). Ulixertinib has also been shown to inhibit A375 cell proliferation with an IC₅₀ value of 180 nM.
Verwenden
Ulixertinib Hydrochloride is an acid salt of Ulixertinib (U700830), a potent and reversible ERK1/ERK2 inhibitor with IC50 of <0.3 nM for ERK2. Inhibits cell proliferation. Anti-cancer.
Verwenden
Ulixertinib hydrochloride is a potent in vitro inhibitor of ERK1/2 kinase that contacts myogenic precursor cells in farmed animals, thereby promoting fusion and myogenic maturation for industrial meat production.
in vitro
in two lymphoma cell lines (sudhl-10 and raji), treatment with ulixertinib significantly reduced the expression of erk1/2 phosphorylation in a dose-dependent manner. treatment with 0.4 nm ulixertinib decreased the percentage of g2-m phase cells in the sudhl-10 cells. in the raji cells, treated with ulixertinib at 0.4 and 1.0 nm increased the percentage of g0-g1 phase cells and decreased s phase cells [1]. treatment of ulixertinib at the dose of 0.1, 0.4 and 1.0 nm for 48 h dose-dependently increased the number of early apoptotic sudhl- 10 and raji cells [1]. in sudhl-10 and raji cells, ulixertinib reduced mrna and protein expression of vegfr2 and bcl-2 genes and increased the expression of bax and caspase-3 genes [1].
in vivo
bvd-523 inhibited tumor growth in braf-mutant melanoma and colorectal xenografts as well as in kras-mutant colorectal and pancreatic models. bvd-523 treatment in combination with dabrafenib inhibited tumor growth in a braf-mutant melanoma model [3]. single-agent bvd-523 inhibited the growth of a patient-derived tumor xenograft harboring cross-resistance to dabrafenib, trametinib, and the combination treatment following clinical progression on a mek inhibitor [3].

Ulixertinib hydrochloride Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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