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Ruxolitinib INCB018424 phosphate

Category:
Pharma
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Description

Description: Ruxolitinib phosphate is an effective and selective JAK1/2 inhibitor with IC50 values of 3.3 nM and 2.8 nM, respectively, and its selectivity is more than 130 times that of JAK3. Ruxolitinib phosphate induces autophagy and kills tumor cells through toxic mitochondrial autophagy.

CAS:1092939-17-7

Molecular formula: C17H21N6O4P

Molecular weight: 404.36

In Vitro study (in vitro study)

Ruxolitinib phosphate effectively and selectively inhibits JAK2V617F-mediated signal transduction and cell proliferation in Ba/F3 cells and HEL cells [1].

Ruxolitinib phosphate significantly increased the apoptosis of Ba/F3 cells in a dose-dependent manner.

Ruxolitinib phosphate(64 nM) doubled the number of mitochondrial depolarization cells in Ba/F3 cells [1].

In Vivo study (in vivo)

In the JAK2V617F-driven mouse model, the survival rate of mice was over 90% after oral administration of 180 mg/kg of Ruxolitinib phosphate twice a day, and the circulating level of splenomegaly and inflammatory cytokines was significantly reduced, and the tumor cells were cleared first, thus significantly prolonging the survival time without bone marrow suppression or immunosuppression [1].

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