R788

Hersteller MedChem Express
Kategorie
Typ Inhibitors
Specific against other
Menge 50mg
ArtNr HY-13038A-50mg
Eclass 6.1 30220300
Eclass 9.0 32160605
Lieferbar
Synonyms
Fostamatinib, R 788, R-788
CAS No.
901119-35-5
Purity
>98%
MW
5804595
Formula
C23H26FN6O9P
Solubility
10 mM in DMSO
Biological Description
R788 (Fostamatinib), a prodrug of the active metabolite R406, is a potent Syk inhibitor with IC50 of 41 nM.
IC50 Value: 41 nM [1]
Target: Syk
in vitro: R788 is a methylene phosphate prodrug of R406, which can be rapidly converted to R406 in vivo. R406 (in vitro active form of R788) selectively inhibits Syk-dependent signaling with EC50 values ranging from 33 nM to 171 nM, more potently than Syk-independent pathways in different cells [1]. R406 inhibits cellular proliferation of a variety of diffuse large B-cell lymphoma (DLBCL) cell lines with EC50 values ranging from 0.8 uM to 8.1 uM [2]. R406 treatment reduces basal phosphorylation of BLNK, Akt, glycogen synthase kinase-3 (GSK-3), forkhead box O (FOXO) and ERK not only in cells with high (TCL-002) but also in cells with low levels of phosphorylated Syk (TCL1-551). In addition, R406 completely inhibits the anti-IgM induced Bcr signal in TCL1 leukemias. Despite the higher levels of constitutively active Syk in TCL1 leukemias, R406 is not selectively cytotoxic to the leukemic cells [3].
in vivo: R788 effectively inhibits BCR signaling in vivo, resulting in reduced proliferation and survival of the malignant B cells and significantly prolonged survival of the treated animals [3].
Publications
Cancer Cell. 2014 Feb 10; 25(2):226-42.
Menge: 50mg
Lieferbar: In stock
Listenpreis: 577,14 €
Rabatt: -10,0%
Preis: 519,43 €
Sie sparen: 57,71 €
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