S-Ruxolitinib (INCB018424) 941685-37-6

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Molecular Weight:

306.37 S-Ruxolitinib is the chirality of INCB018424, which is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM, >130-fold selectivity for JAK1/2 versus JAK3. Phase 3.


Biological Activity


INCB018424 potently and selectively inhibits JAK2V617F-mediated
signaling and proliferation in Ba/F3 cells and HEL cells. INCB018424
markedly increases Apoptosis in a dose dependent manner in Ba/F3 cells.
INCB018424 (64 nM) results in a doubling of cells with depolarized
mitochondria in Ba/F3 cells. INCB018424 inhibits proliferating of
erythroid progenitors from normal donors and polycythemia vera patients
with IC50 of 407 nM and 223 nM, respectively. INCB018424 demonstrates
remarkable potency against erythroid colony formation with IC50 of 67nM.


INCB018424 (180 mg/kg, orally, twice a day) results in survive rate of
greater than 90% by day 22 in a JAK2V617F-driven mouse model. INCB018424
(180 mg/kg, orally, twice a day) markedly reduces splenomegaly and
circulating levels of inflammatory cytokines, and preferentially
eliminated neoplastic cells, resulting in significantly prolonged
survival without myelosuppressive or immunosuppressive effects in a
JAK2V617F-driven mouse model.


The primary end point is
reached in 41.9% of patients in the Ruxolitinib group as compared with
0.7% in the placebo group in the double-blind trial of myelofibrosis.
Ruxolitinib results in maintaining of reduction in spleen volume and
improvement of 50% or more in the total symptom score.


A
total of 28% of the patients in the Ruxolitinib (15 mg twice daily)
group has at least a 35% reduction in spleen volume at week 48 in
patients with myelofibrosis, as compared with 0% in the group receiving
the best available therapy. The mean palpable spleen length has
decreased by 56% with Ruxolitinib but has increased by 4% with the best
available therapy at week 48. Patients in the ruxolitinib group has an
improvement in overall quality-of-life measures and a reduction in
symptoms associated with myelofibrosis.

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Product Categories : Epigenetics > JAK Inhibitor