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Ruxolitinib sulfate

Catalog No. T61988 CAS 1092939-16-6

Ruxolitinib sulfate (INCB018424 sulfate) is a potent, selective JAK1/2 inhibitor with IC 50 s of 3.3 nM/2.8 nM. Ruxolitinib sulfate shows < 130-fold selectivity for JAK1/2 versus JAK3.

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Ruxolitinib sulfate, CAS 1092939-16-6

Pack Size	Availability	Price/USD
25 mg	8-10 weeks	$ 1,520.00
50 mg	8-10 weeks	$ 1,980.00
100 mg	8-10 weeks	$ 2,500.00

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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

Biological Description

Chemical Properties

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Description	Ruxolitinib sulfate (INCB018424 sulfate) is a potent, selective JAK1/2 inhibitor with IC 50 s of 3.3 nM/2.8 nM. Ruxolitinib sulfate shows > 130-fold selectivity for JAK1/2 versus JAK3.
In vitro	Ruxolitinib sulfate (INCB018424 sulfate) effectively and selectively hampers JAK2V617F-mediated signaling and cell growth, significantly boosts apoptosis in a dose-dependent manner, and achieves a twofold increase in cells with depolarized mitochondria at a concentration of 64 nM in Ba/F3 cells. It also exhibits exceptional efficacy in inhibiting erythroid colony formation, noted by an IC50 of 67 nM. Moreover, it suppresses the proliferation of erythroid progenitors from both healthy individuals and patients with polycythemia vera, as evidenced by IC50 values of 407 nM and 223 nM, respectively [1].
In vivo	Ruxolitinib (INCB018424 sulfate; 180 mg/kg, orally, twice daily) demonstrates over a 90% survival rate by day 22 and significantly reduces splenomegaly and inflammatory cytokine levels in a JAK2V617F-driven mouse model; it effectively targets and eradicates neoplastic cells without causing myelosuppression or immunosuppression [1]. In myelofibrosis patients within a double-blind trial, 41.9% achieved the primary endpoint with Ruxolitinib treatment versus only 0.7% in the placebo group, highlighting its efficacy in spleen volume reduction and symptom improvement [2]. Furthermore, 28% of patients receiving Ruxolitinib (15 mg twice daily) experienced at least a 35% decrease in spleen volume by week 48, a stark contrast to none in the best available therapy group, accompanied by a 56% reduction in mean palpable spleen length versus a 4% increase with alternative treatments. Ruxolitinib also significantly enhances overall quality-of-life and reduces myelofibrosis symptoms [3].

Molecular Weight	404.45
Formula	C17H20N6O4S
CAS No.	1092939-16-6

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Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Ruxolitinib sulfate 1092939-16-6 inhibitor inhibit

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