Ruxolitinib sulfate (INC 424, INCB 18424, INCB 018424, Jakafi, Jakavi)

Alias: INCB-018424 sulfate, INCB 018424, INCB018424; INC424, INC424, INC-424; INCB18424, INCB 18424, INCB-18424; Jakafi and Jakavi (trade name)
Cat No.:V0077 Purity: ≥98%
Ruxolitinib sulfate, the sulfate salt of ruxolitinib which isalso known as Jakafi, Jakavi, INC-424, INCB-18424 or INCB-018424, is the first-in class, potent, selective, and orally bioavailable JAK1/2 (Janus-associated kinase) inhibitor with IC50 of 3.3 nM/2.8 nM in cell-free assays, it exhibits >130-fold selectivity for JAK1/2 versus JAK3.
Ruxolitinib sulfate (INC 424, INCB 18424, INCB 018424, Jakafi, Jakavi) Chemical Structure CAS No.: 1092939-16-6
Product category: JAK
This product is for research use only, not for human use. We do not sell to patients.
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Other Forms of Ruxolitinib sulfate (INC 424, INCB 18424, INCB 018424, Jakafi, Jakavi):

  • Ruxolitinib (INCB-018424; INC-424)
  • S-Ruxolitinib (INCB-018424)
  • Ruxolitinib Phosphate (INC-424, INCB-18424, INCB-018424, Jakafi and Jakavi)
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Ruxolitinib sulfate, the sulfate salt of ruxolitinib which is also known as Jakafi, Jakavi, INC-424, INCB-18424 or INCB-018424, is the first-in class, potent, selective, and orally bioavailable JAK1/2 (Janus-associated kinase) inhibitor with IC50 of 3.3 nM/2.8 nM in cell-free assays, it exhibits >130-fold selectivity for JAK1/2 versus JAK3. Ruxolitinib has potential antineoplastic and immunomodulating activities. It was approved in 2011 by FDA for the treatment of intermediate or high-risk myelofibrosis.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
Ruxolitinib sulfate (INCB018424 sulfate) significantly and selectively enhances apoptosis in a dose-dependent manner, potently and selectively inhibits JAK2V617F-mediated signaling and proliferation, and causes a doubling of cells with depolarized mitochondria in Ba/F3 cells at 64 nM. With an IC50 of 67 nM, roxolitinib exhibits significant effectiveness against the development of erythroid colonies. It also suppresses the proliferation of erythroid progenitors from both normal donors and patients with polycythemia vera, with IC50 values of 407 nM and 223 nM, respectively[1].
ln Vivo
Ruxolitinib (INCB018424 sulfate; 180 mg/kg, orally, twice a day) causes a JAK2V617F-driven mouse model to exhibit a significantly prolonged survival without myelosuppressive or immunosuppressive effects. By day 22, it also significantly reduces inflammatory cytokine levels and splenomegaly and preferentially eliminates neoplastic cells[1]. In the double-blind trial of myelofibrosis, 41.9% of patients in the Ruxolitinib group and 0.7% in the placebo group reach the primary end point. Ruxolitinib causes the overall symptom score to improve by 50% or more while maintaining the reduction in spleen volume[2]. When given roxolitinib (15 mg twice daily), patients with myelofibrosis had a reduction in spleen volume of at least 35% in 28% of cases by week 48, compared to 0% in the group receiving the best available therapy. By week 48, the mean palpable spleen length had increased by 4% with the best available therapy, but had dropped by 56% with Ruxolitinib. Patients receiving ruxolitinib showed improvements in overall quality-of-life metrics as well as a decrease in myelofibrosis-related symptoms[3].
Animal Protocol
Dissolved in 5% dimethyl acetamide, 0.5% methocellulose; 180 mg/kg/day; Oral gavage
JAK2V617F-driven mouse model
References
[1]. Quintas-Cardama A, et al. Preclinical characterization of the selective JAK1/2 inhibitor INCB018424: therapeutic implications for the treatment of myeloproliferative neoplasms. Blood, 2010, 115(15), 3109-3117.
[2]. Verstovsek S, et al. A double-blind, placebo-controlled trial of ruxolitinib for myelofibrosis. N Engl J Med, 2012, 366(9), 799-807.
[3]. Harrison C, et al. JAK inhibition with ruxolitinib versus best available therapy for myelofibrosis. N Engl J Med. 2012 Mar 1;366(9):787-98
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C17H18N6.H2O4S
Molecular Weight
404.4435
CAS #
1092939-16-6
SMILES
[H][C@@](C1CCCC1)(N2N=CC(C3=C4C=CNC4=NC=N3)=C2)CC#N.O=S(O)(O)=O
Synonyms
INCB-018424 sulfate, INCB 018424, INCB018424; INC424, INC424, INC-424; INCB18424, INCB 18424, INCB-18424; Jakafi and Jakavi (trade name)
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: >50 mg/mL
Water:<1 mg/mL
Ethanol:<1 mg/mL
Solubility (In Vivo)
2% DMSO+30% PEG 300+ddH2O:5mg/mL
 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.4726 mL 12.3628 mL 24.7255 mL
5 mM 0.4945 mL 2.4726 mL 4.9451 mL
10 mM 0.2473 mL 1.2363 mL 2.4726 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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Biological Data
  • Ruxolitinib sulfate

    INCB018424 (Ruxolitinib)treatment improves viability and splenomegaly in a JAK2V617F-driven model of malignant disease.Blood.2010 Apr 15;115(15):3109-17.


    Ruxolitinib sulfate

  • Ruxolitinib sulfate

    Macroscopic and microscopic effects of INCB018424 on spleens from mice inoculated with Ba/F3-EpoR-JAK2V617F cells.Blood.2010 Apr 15;115(15):3109-17.

  • Ruxolitinib sulfate

    INCB018424 does not affect normal hematologic parameters.Blood.2010 Apr 15;115(15):3109-17.

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