Fedratinib-d9

Fedratinib-d9 (TG-101348-d9) is deuterium labeled Fedratinib. Fedratinib (TG-101348) is a potent, selective, ATP-competitive and orally active JAK2 inhibitor with IC50s of 3 nM for both JAK2 and JAK2V617F kinase. Fedratinib shows 35- and 334-fold selectivity over JAK1 and JAK3, respectively. Fedratinib induces cancer cell apoptosis and has the potential for myeloproliferative disorders research[1][2][3].

Product Specifications

Product Name Alternative

TG-101348-d9; SAR 302503-d9

UNSPSC

12352005

Target

Apoptosis; Isotope-Labeled Compounds; JAK

Type

Isotope-Labeled Compounds

Related Pathways

Apoptosis; Epigenetics; JAK/STAT Signaling; Others; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Smiles

O=S(C1=CC=CC(NC2=NC(NC3=CC=C(OCCN4CCCC4)C=C3)=NC=C2C)=C1)(NC(C([2H])([2H])[2H])(C([2H])([2H])[2H])C([2H])([2H])[2H])=O

Molecular Formula

C27H27D9N6O3S

Molecular Weight

533.73

References & Citations

[1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53 (2) :211-216.|[2]Geron I, et al. Selective inhibition of JAK2-driven erythroid differentiation of polycythemia vera progenitors. Cancer Cell. 2008 Apr;13 (4) :321-30.|[3]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.