Fedratinib

Bezeichnung:Fedratinib

CAS-Nr936091-26-8

Englisch Name:Fedratinib

CBNumberCB12485002

SummenformelC27H36N6O3S

Molgewicht524.68

MOL-Datei936091-26-8.mol

Fedratinib physikalisch-chemischer Eigenschaften

Schmelzpunkt	180-182°C
Siedepunkt	713.7±70.0 °C(Predicted)
Dichte	1.247
storage temp.	Keep in dark place,Inert atmosphere,Store in freezer, under -20°C
Löslichkeit	DMSO (Slightly), Methanol (Slightly)
Aggregatzustand	Beige powder.
pka	11.95±0.50(Predicted)
Farbe	White to Off-White
CAS Datenbank	936091-26-8

Sicherheit

HS Code

29350090

Gefahreninformationscode (GHS)

Fedratinib Chemische Eigenschaften,Einsatz,Produktion Methoden

Charakteristisch
Class: non-receptor tyrosine kinase
Treatment: myeloproliferative diseases
Oral bioavailability = 18–37%
Elimination half-life = 2–3 days
Protein binding = 91–96%
Verwenden
TG101348 is a selective inhibitor of JAK2 tyrosine kinase. Potent JAK2 inhibitor.
Verwenden
A potent, highly selective and ATP-competitive JAK2 inhibitor with an IC50 of 3 nM for JAK2 and JAK2V617F.
Definition
ChEBI: N-tert-butyl-3-[[5-methyl-2-[4-[2-(1-pyrrolidinyl)ethoxy]anilino]-4-pyrimidinyl]amino]benzenesulfonamide is a sulfonamide.
Biologische Aktivität
tg101348, also known as sar302503, is a potent and selective inhibitor of janus kinase 2 (jak2), one member of a family of 4 cytoplasmic tyrosine kinases including janus kinase 1(jak1), jak2, janus kinase 3 (jak3) and tyrosine kinase 2 (tyk2), with the inhibition constant ic50 of 3 nm. comparing to other close related kinases, the selectivity of tg101348 for jak2 is 35- and 334-fold stronger than that for jak3 and jak1 respectively. tg10348 is capable of inducing apoptosis in hel cells as well baf/3 cells harboring jak2v617 mutation and inhibiting hematopoietic progenitor colony formation and erythroid engraftment in samples from polycythemia vera (pv) patients.srdan verstovsek. therapeutic potential of jak2 inhibitors. hematology am soc hematol educ program 2009:636-642
Pharmakokinetik
Fedratinib pharmacokinetics are characterized by prolonged duration of action: effective half-life of 41 hours, terminal half-life of approximately 114 hours, and elimination half-life of 2–3 days, which makes it suitable for once-daily dosing. In contrast, ruxolitinib has a short terminal half-life of approximately 3 h, suggesting that twice-daily administration of ruxolitinib is more suitable than once-daily dosing. Following oral administration, fedratinib is mainly bio-oxidized by CYP3A4 to give two major circulating metabolites in the plasma: the pyrrolidone derivative 1 and the N-butyric acid 2.
target
JAK2

Fedratinib Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

936091-26-8, Fedratinib Verwandte Suche:

Send Inquriy