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 inhibit the proliferation of erythroid progenitor cells derived from both healthy donors and patients with polycythemia vera, with IC50 Values of 407 nM and 2 23 nM, respectively furthermore , INCB018424 demonstrates potent activity in inhibitin 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 an 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 ove All improvement in quality of life and a reduction in symptoms associated with myelofibrosis. Read more...
Cell Research	Cell lines: Ba/F3 and HEL cells. concentration : 3 μM. Method: Cells are seeded at × 0^3 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 usin 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 o 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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