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Ruxolitinib

SKU: orb1307364

Description

Ruxolitinib

Research Area

Cardiovascular Research, Cell Biology, Epigenetics & Chromatin, Signal Transduction, Stem Cell & Developmental Biology

Images & Validation

Key Properties

CAS Number941678-49-5
MW306.36
Purity99.99%
FormulaC17H18N6
SMILESN#CC[C@H](C1CCCC1)n1cc(cn1)-c1ncnc2[nH]ccc12
TargetJAK,Apoptosis,Mitophagy,Tyrosine Kinases,Autophagy
Solubility10% DMSO+40% PEG300+5% Tween 80+45% Saline:5.7 mg/mL (18.61 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble);DMSO:242 mg/mL (789.92 mM);H2O:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

Target IC50
JAK2:2.8 nM (cell free)|JAK1:3.3 nM (cell free)|TYK2:19 nM (cell free)|JAK3:428 nM
In Vivo
METHODS: To assay antitumor activity in vivo Ruxolitinib (3-30 mg/kg, 5% dimethyl acetamide, 0.5% methocellulose) was administered by gavage to BAL-/- mice harborin the tumor Ba/F3-JAK2V617F twice daily for three weeks. Results: Ruxolitinib significantly reduced splenomegaly and circulating levels of inflammatory cytokines and preferentially eliminated tumor cells, resulting in significantly prolonged survival without myelosuppressive or immunosuppressive effects. METHODS: To assay antitumor activity in vivo Ruxolitinib (150 mg/kg) was orally administered to BALB/c nude mice bearin the human colorectal tumor LS411N every two days for two weeks. Results: Oral administration of Ruxolitinib significantly inhibite the growth of human colorectal tumors in vivo without causing hepatotoxicity.
In Vitro
METHODS: Ba/F3-EpoR-JAK2V617F cells were treated with Ruxolitinib (0-10 μM) for 48 h. Cell viability was measured using Cell-Titer Glo. Results: Ruxolitinib dose-dependently decreased cell viability with an IC50 of 126 nM METHODS: Hodgkin's lymphoma cells HDLM-2 were treated with Ruxolitinib (10-100 nM) for 24 h, an the expression levels of target proteins were detected by Western Blot. Results: Ruxolitinib significantly inhibite the downstream activities of p-STAT3 and p-STAT5 in a dose-dependent manner, while total STAT3 and STAT5 levels remained unchanged.
Cell Research
Cells were seeded at 2000/well of white bottom 96-well plates, treated with compounds from DMSO stocks (0.2% final DMSO concentration , and incubated for 48 hours at 37℃ith 5% CO2. Viability was measured by cellular ATP determination usin the Cell-Titer Glo luciferase reagent or viable cell counting. Values were transformed to percent Inhibition relative to Vehicle control, and IC50 curves were fitted according to nonlinear regression analysis o the data using PRISM GraphPad.
Animal Research
All o the procedures were conducted in accordance wit the US Public Health Service Policy on Humane Care and Use of Laboratory Animals. Mice were fed s andard rodent chow and provided with water ad libitum. Ba/F3-JAK2V617F cells (10^5 per mouse) were inoculated intravenously into 6- to 8-week-old f Male BAL-/- mice. Survival was monitored daily, and moribund mice were humanely killed and considered deceased at time of death. Treatment with Vehicle (5% dimethylacetamide, 0.5% methocellulose) or INCB018424 began within 24 hours of cell inoculation, twice daily by oral gavage. Hematologic parameters were measured using a Bayer Advia120 analyzed, and statistical significance was determined using Dunnett testing.

Storage & Handling

Storagestore at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

Janus kinase, JAK1, JAK2, JAK, inhibit, INCB018424, INCB-018424, INCB 18424, INCB18424, INCB-18424, INCB 018424, Mitochondrial Autophagy, Mitophagy, Inhibitor, (R)-Ruxolitinib, Apoptosis, Autophagy, Ruxolitinib, Tyk2, TyrosineKinases, Tyrosine Kinases

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Quality Guarantee

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Key Properties

No computed properties available.

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Ruxolitinib (orb1307364)

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% Tween 80 +
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Available Sizes

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1 ml x 10 mM (in DMSO)
¥ 1,300.00
5 mg
¥ 1,300.00
10 mg
¥ 1,430.00
25 mg
¥ 1,820.00
50 mg
¥ 2,080.00
100 mg
¥ 2,600.00
200 mg
¥ 3,900.00
500 mg
¥ 6,240.00
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