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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

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Ruxolitinib

Key Properties

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CAS Number941678-49-5
MW306.36
Purity99.99%
FormulaC17H18N6
SMILESN#CC[C@H](C1CCCC1)n1cc(cn1)-c1ncnc2[nH]ccc12
TargetJAK,Mitophagy,Apoptosis,Autophagy,Tyrosine Kinases
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

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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 BALB/c mice harboring 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 bearing the human colorectal tumor LS411N every two days for two weeks. RESULTS: Oral administration of Ruxolitinib significantly inhibited the growth of human colorectal tumors in vivo without causing hepatotoxicity.
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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, and the expression levels of target proteins were detected by Western Blot. RESULTS: Ruxolitinib significantly inhibited the downstream activities of p-STAT3 and p-STAT5 in a dose-dependent manner, while total STAT3 and STAT5 levels remained unchanged.
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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°C with 5% CO2. Viability was measured by cellular ATP determination using 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 of the data using PRISM GraphPad .
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Animal Research
All of the procedures were conducted in accordance with the US Public Health Service Policy on Humane Care and Use of Laboratory Animals. Mice were fed standard 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 female BALB/c 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 .
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Storage & Handling

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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

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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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Compound Identifiers

PubChem CID
25126798 ↗

Key Properties

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No computed properties available.

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Ruxolitinib (orb1307364)

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1 ml x 10 mM (in DMSO)
$ 100.00
5 mg
$ 100.00
10 mg
$ 110.00
25 mg
$ 140.00
50 mg
$ 160.00
100 mg
$ 200.00
200 mg
$ 300.00
500 mg
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