AG 490

Bezeichnung:AG 490

CAS-Nr133550-30-8

Englisch Name:AG 490

CBNumberCB4779212

SummenformelC17H14N2O3

Molgewicht294.3

MOL-Datei133550-30-8.mol

AG 490 physikalisch-chemischer Eigenschaften

Schmelzpunkt	215°C(lit.)
Siedepunkt	615.2±55.0 °C(Predicted)
Dichte	1.337
storage temp.	-20°C
Löslichkeit	ethanol: 5 mg/mL
Aggregatzustand	solid
pka	8.75±0.10(Predicted)
Farbe	yellow
Stabilität	Stable for 1 year from date of purchase as supplied. Solutions in DMSO, DMF, or ethanol may be stored at -20°C for up to 1 month.
InChIKey	TUCIOBMMDDOEMM-ZSOIEALJSA-N

Sicherheit

Kennzeichnung gefährlicher	Xi,N,T
R-Sätze:	36/37/38-50-25
S-Sätze:	26-36-61-45
RIDADR	UN2811 - class 6.1 - PG 3 - EHS - Toxic solids, organic, n.o.s., HI: all
WGK Germany	1
RTECS-Nr.	UC6316197
HazardClass	6.1
PackingGroup	III
HS Code	29269090

Gefahreninformationscode (GHS)

AG 490 Chemische Eigenschaften,Einsatz,Produktion Methoden

R-Sätze Betriebsanweisung:
R36/37/38:Reizt die Augen, die Atmungsorgane und die Haut.
S-Sätze Betriebsanweisung:
S26:Bei Berührung mit den Augen sofort gründlich mit Wasser abspülen und Arzt konsultieren.
S36:DE: Bei der Arbeit geeignete Schutzkleidung tragen.
Beschreibung
AG-490 (133550-30-8) is a potent inhibitor of the JAK2 tyrosine kinase. In acute lymphoblastic leukemia (ALL) cells, which abundantly express JAK-2, AG-490 dose-dependently blocked cell growth, induced apoptosis and inhibited DNA synthesis. Blocks the growth of all pre-B ALL cells with no effect on normal B or T cells. Does not significantly inhibit other kinases such as Lck, Lyn, Btk, Syk and Src. Reduces liver injury in LPS-induced shock.3 AG-490 is a useful tool for exploring the role of JAK2/STAT3 pathway in physiologic processes.4
Verwenden
AG 490 is a potent epidermal growth factor receptor kinase autophosphorylation inhibitor with an IC50 of 100 nM and 56.8 μM for EGFR and JAK, respectively.
Verwenden
Tyrphostin AG has been used to block IL-6 cytokine signaling to study its effects on glial cell reactivity⁵. AG 490 has also been used as a JAK2 inhibitor in human umbilical vein endothelial cells⁶.
Definition
ChEBI: Tyrphostin B42 is a monocarboxylic acid amide obtained by formal condensation of the carboxy group of (2E)-2-cyano-3-(3,4-dihydroxyphenyl)prop-2-enoic acid with the amino group of benzylamine. It has a role as an EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor, an antioxidant, a STAT3 inhibitor, an anti-inflammatory agent, an apoptosis inducer and a geroprotector. It is an enamide, a monocarboxylic acid amide, a nitrile, a member of catechols and a secondary carboxamide.
Biologische Aktivität
Selective inhibitor of EGF receptor tyrosine kinase (IC 50 values are 2 and 13.5 μ M for EGFR and ErbB2 respectively). Inhibitor of JAK2, JAK3/STAT, JAK3/AP-1 and JAK3/MAPK pathways and potently inhibits cytokine-independent cell growth in vitro and tumor cell invasion in vivo .
Biochem/physiol Actions
Jak-2 protein tyrosine kinase (PTK) inhibitor. Inhibits interleukin 2 (IL-2) driven mitogenesis and triggers apoptosis of tumor cells in Sezary syndrome, a leukemic variant of cutaneous T cell lymphoma.
Lager
Room temperature
Einzelnachweise
References/Citations 1) Wang et al. (1999), JAK3, STAT, and MAPK signaling pathways as novel molecular targets for the tyrphostin AG-490 regulation of IL-2-mediated T cell response; J. Immunol. 162 3897 2) Meydan et al. (1996), Inhibition of acute lymphoblastic leukaemia by Jak-2 inhibitor; Nature, 379 645 3) Gyurkovska and Ivanovaska (2015), Tyrosine kinase inhibitor tyrphostin AG490 reduces liver injury in LPS-induced shock; Eur. J. Pharmacol., 751 118 4) Wu et al. (2015), ROS generated during early reperfusion contribute to intermittent hypobaric hypoxia-afforded cardioprotection against postischemia-induced Ca(+2) overload and contractile dysfunction via the JAK2/STAT3 pathway; J. Mol. Cell. Cardiol., 81 150

AG 490 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

133550-30-8, AG 490 Verwandte Suche:

Send Inquriy