Fedratinib hydrochloride hydrate (Synonyms: TG-101348 hydrochloride hydrate; SAR 302503 hydrochloride hydrate) |
| Catalog No.GC60161 |
Le chlorhydrate de fédratinib hydraté (TG-101348 chlorhydrate hydraté) est un inhibiteur de JAK2 puissant, sélectif, compétitif pour l'ATP et actif par voie orale avec des CI50 de 3 nM pour les kinases JAK2 et JAK2V617F. L'hydrate de chlorhydrate de fédratinib présente une sélectivité de 35 et 334 fois par rapport À JAK1 et JAK3, respectivement. L'hydrate de chlorhydrate de fédratinib induit l'apoptose des cellules cancéreuses et a le potentiel pour la recherche sur les troubles myéloprolifératifs.
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Cas No.: 1374744-69-0
Sample solution is provided at 25 µL, 10mM.
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Fedratinib hydrochloride hydrate (TG-101348 hydrochloride hydrate) is a potent, selective, ATP-competitive and orally active JAK2 inhibitor with IC50s of 3 nM for both JAK2 and JAK2V617F kinase. Fedratinib hydrochloride hydrate shows 35- and 334-fold selectivity over JAK1 and JAK3, respectively. Fedratinib hydrochloride hydrate induces cancer cell apoptosis and has the potential for myeloproliferative disorders research[1][2].
Fedratinib (TG101348) inhibits proliferation of a human erythroblast leukemia (HEL) cell line that harbors the JAK2V617F mutation, as well as a murine pro-B cell line expressing human JAK2V617F (Ba/F3 JAK2V617F), with an IC50 value of approximately 300 nM for either line. Proliferation of parental Ba/F3 cells was inhibited to a comparable level, with an IC50 value of ∼420 nM[1]. Exposure of these cells to Fedratinib (TG101348) (0.1 μM, 0.3 μM, 1 μM, 3 μM, and 10 μM) reduces STAT5 phosphorylation at concentrations that parallel the concentrations required to inhibit cell proliferation[1]. Fedratinib (TG101348) (0.1 μM, 0.3 μM, 1 μM, 3 μM, and 10 μM) induces apoptosis in both HEL and Ba/F3 JAK2V617F cells in a dose-dependent manner[1].
Fedratinib (TG101348; 60-120 mg/kg; oral gavage; twice daily; for 42 days; C57Bl/6 mice) trewatment shows a dose-dependent reduction in polycythemia and a marked dose-dependent reduction in splenomegaly of treated animals[1]. Animal Model: C57Bl/6 mice induced by the JAK2V617F mutation[1]
[1]. Wernig G, et al. Efficacy of TG101348, a selective JAK2 inhibitor, in treatment of a murine model of JAK2V617F-induced polycythemia vera. Cancer Cell. 2008 Apr;13(4):311-20. [2]. Geron I, et al. Selective inhibition of JAK2-driven erythroid differentiation of polycythemia vera progenitors. Cancer Cell. 2008 Apr;13(4):321-30.
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