AZ 628

Bezeichnung:AZ 628

CAS-Nr878739-06-1

Englisch Name:AZ 628

CBNumberCB22516246

SummenformelC27H25N5O2

Molgewicht451.52

MOL-Datei878739-06-1.mol

AZ 628 physikalisch-chemischer Eigenschaften

Dichte	1.21±0.1 g/cm3(Predicted)
storage temp.	-20°C
Löslichkeit	DMSO: soluble10mg/mL, clear
Aggregatzustand	powder
pka	12.92±0.70(Predicted)
Farbe	white to beige

Sicherheit

Kennzeichnung gefährlicher	T
R-Sätze:	25-36/37/38
S-Sätze:	26-36/37/39-45
RIDADR	UN 2811 6.1 / PGIII
WGK Germany	3
HS Code	2922500090

Gefahreninformationscode (GHS)

AZ 628 Chemische Eigenschaften,Einsatz,Produktion Methoden

Verwenden
AZ 628 is an inhibitor of B-RAF and B-RAF(V600E)
Definition
ChEBI: 3-(2-cyanopropan-2-yl)-N-[4-methyl-3-[(3-methyl-4-oxo-6-quinazolinyl)amino]phenyl]benzamide is a member of benzamides.
Biologische Aktivität
az628 is a potent and newly discorvered inhibitor of braf, c-raf-1 and brafv600e with ic50 values of 105 nm, 29 nm and 34 nm, respectively. this compound prevents craf activation through persistently occupying the atp-binding site of raf kinase. specificity profile suggests that az628 also inhibits activation of other tyrosine protein kinases such as ddr2, vegfr2, lyn, flt1, fms and others.raf kinases a family of three serine/threonine-specific protein kinases and participate in the ras-raf-mek-erk signal transduction cascade, also known as the mitogen-activated protein kinase (mapk) cascade. the activation of mapk signaling leads to different cellular response such as cell proliferation, apoptosis and inflammation.az628 has the potent anti-tumor activity. in human colon and melanoma-derived cell line that carries the recurrent v600e activating braf mutation, az628 was shown to inhibit anchorage-dependent and -independent growth, induce cell cycle arrest, and cause apoptosis [1]. az628 may be antiangiogenic due to inhibition of vegfr2 [2].generation of melanoma cell line clones is obtained resistance to the raf kinase inhibitor az628. resistance to az628 is connected with raised levels of the raf downstream effector p-erk1/2. erk1/2 initiation in az628-resistant clones is interceded by mek. supported multiplication of az628-resistant clones is to a great extent autonomous of braf kinase action. az628-resistant clones express elevated craf. survival of az628-safe cells is subject to craf [1].
in vitro

AZ628 inhibits B-Raf, B-Raf AZ628 acts on B-Raf-containing M14 parental cell lines treated with increasing concentrations of AZ628, an effective inhibition of p-ERK1/2 levels was observed. It acts on AZ628-resistant M14 cells and does not inhibit ERK activation. AZ628 acts on NRAS-mutated malignant melanoma cells and effectively reduces ERK activation.
target

Target Value
C-Raf-1
(Cell-free assay) 29 nM
B-Raf (V600E)
(Cell-free assay) 34 nM
B-Raf
(Cell-free assay) 105 nM
Lager
Store at +4°C
Einzelnachweise
1. montagut c, sharma sv, shioda t, mcdermott u, ulman m, ulkus le, et al. elevated craf as a potential mechanism of acquired resistance to braf inhibition in melanoma. cancer res 2008,68:4853-4861.2. khazak v, astsaturov i, serebriiskii ig, golemis ea. selective raf inhibition in cancer therapy. expert opin ther targets 2007,11:1587-1609.

AZ 628 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

Send Inquriy

Target	Value
C-Raf-1 (Cell-free assay)	29 nM
B-Raf (V600E) (Cell-free assay)	34 nM
B-Raf (Cell-free assay)	105 nM