Ruxolitinib (S enantiomer)

SKU: orb1301027

Description

Research Area

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

Images & Validation

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Key Properties

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CAS Number	941685-37-6
MW	306.36
Purity	99.79%
Formula	C₁₇H₁₈N₆
SMILES	N#CC[C@@H](C1CCCC1)n1cc(cn1)-c1ncnc2[nH]ccc12
Target	JAK,Tyrosine Kinases
Solubility	DMSO:57 mg/mL (186.06 mM);Ethanol:57 mg/mL (186.06 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (6.53 mM);H2O:5 mg/mL (16.32 mM)

Bioactivity

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Target IC50	TYK2 (Cell-free assay):19 nM\|JAK1 (cell-free assay):3.3 nM\|JAK2 (cell-free assay):2.8 nM
In Vivo	INCB018424 significantly induces apoptosis in Ba/F3 cells in a dose-dependent manner and effectively and selectively inhibits JAK2V617F-mediated signaling and proliferation in both Ba/F3 and HEL cells. At a concentration of 64 nM, INCB018424 doubles mitochondrial depolarization in Ba/F3 cells. It inhibits the proliferation of erythroid progenitor cells derived from both healthy donors and patients with polycythemia vera, with IC50 values of 407 nM and 223 nM, respectively. Furthermore, INCB018424 demonstrates potent activity in inhibiting the formation of erythroid colonies, with an IC50 of 67 nM. Read more...
In Vitro	INCB018424 (180 mg/kg, orally, twice daily) significantly reduced spleen enlargement and the circulation of inflammatory cytokines in a JAK2V617F-driven mouse model, preferentially targeting and eliminating tumor cells, notably prolonging survival without causing bone marrow suppression or immunosuppression. The survival rate exceeded 90% on Day 22 for these mice. Additionally, in myelofibrosis patients, a 15 mg dosage of Ruxolitinib administered twice daily for 48 weeks resulted in at least a 35% reduction in spleen volume in 28% of patients. Patients in the Ruxolitinib group experienced an overall improvement in quality of life and a reduction in symptoms associated with myelofibrosis. Read more...
Cell Research	Cell lines: Ba/F3 and HEL cells. Concentrations: 3 μM. Method: Cells are seeded at 2×103/well of white bottom 96-well plates,treated with INCB018424 from DMSO stocks (0.2% final DMSO concentration),and incubated for 48 hours at 37 ℃ in an atmosphere containing 5% CO2.Viability is measured by cellular ATP determination using the Cell-Titer Glo luciferase reagent or viable cell counting.Values are transformed to percent inhibition relative to vehicle control,and IC50 curves are fitted according to nonlinear regression analysis of the data using PRISM GraphPad. Read more...
Animal Research	Animal Models: JAK2V617F-driven mouse modelFormulation & . Dosages: 5% dimethyl acetamide,0.5% methylcellulose.180 mg/kg. Administration: Oral gavage

Storage & Handling

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Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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Ruxolitinib, Ruxolitinib (S enantiomer), Ruxolitinib S enantiomer, S-Ruxolitinib, S-INCB18424, Tyrosine Kinases, TyrosineKinases, Tyk2, INCB18424, INCB-18424, INCB 018424, INCB-018424, INCB018424, INCB 18424, Janus kinase, JAK, JAK1, JAK2, inhibit, Inhibitor

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Compound Identifiers

PubChem CID

50878566 ↗

Key Properties

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No computed properties available.

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