LY2784544

Hersteller MedChem Express
Kategorie
Typ Inhibitors
Specific against other
Clon N/A
Menge 5mg
ArtNr HY-13034-5mg
Eclass 6.1 30220300
Eclass 9.0 32160605
Lieferbar
Synonyms
LY 2784544, LY-2784544, gandotinib
CAS No.
1229236-86-5
Purity
>98%
MW
4699423
Formula
C23H25ClFN7O
Solubility
10 mM in DMSO
Biological Description
LY2784544 is a potent JAK2 inhibitor with IC50 of 3 nM. LY2784544 also inhibits FLT3, FLT4, FGFR2, TYK2, and TRKB with IC50 of 4, 25, 32, 44, and 95 nM.


IC50 & Target: IC50: 2.52+/-0.49 nM (JAK2), 19.8+/-3 nM (JAK1), 48+/-14.9 nM (JAK3), 4 nM (FLT3), 32 nM (FGFR2)[1]
In Vitro: LY2784544, a potent, selective and ATP-competitive inhibitor of janus kinase 2 (JAK2) tyrosine kinase. LY2784544 effectively inhibits JAK2V617F-driven signaling and cell proliferation in Ba/F3 cells (IC50=20 and 55 nM, respectively). In comparison, LY2784544 is much less potent at inhibiting interleukin-3-stimulated wild-type JAK2-mediated signaling and cell proliferation (IC50=1183 and 1309 nM, respectively). LY2784544 potently inhibits the JAK2V617F signaling (IC50=20 nM) but, remarkably, shows very minimal activity against the IL-3-activated wild-type JAK2 signaling with an IC50 of 1183 nM. LY2784544 inhibits the proliferation of JAK2V617F-expressing cells (IC50=55 nM) and is markedly less potent as an inhibitor of the proliferation of IL-3-stimulated wild-type JAK2 expressing Ba/F3 cells (IC50=1309 nM). LY2784544 is potent in the cell-based TF-1 JAK2 assay (IC50=45 nM) and had the desired threshold selectivity in the NK-92 JAK3/JAK1 heterodimer assay (942 nM)[1].
In Vivo: LY2784544 effectively inhibits STAT5 phosphorylation in Ba/F3-JAK2V617F-GFP (green fluorescent protein) ascitic tumor cells (TED50=12.7 mg/kg) and significantly reduces (P<0.05) Ba/F3-JAK2V617F-GFP tumor burden in the JAK2V617F-induced MPN model (TED50=13.7 mg/kg, twice daily)[1].
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Sicherheitsdatenblatt

HY-13034-5mg.pdf

Menge: 5mg
Lieferbar: In stock
Listenpreis: 178,57 €
Rabatt: -10,0%
Preis: 160,71 €
Sie sparen: 17,86 €
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