Ruxolitinib Phosphate (INC-424, INCB-18424, INCB-018424, Jakafi and Jakavi)

Alias: INCB-018424 phosphate, INCB 018424, INCB018424; INC424, INC424, INC-424; INCB18424, INCB 18424, INCB-18424; Jakafi and Jakavi (trade name)
Cat No.:V0076 Purity: ≥98%
Ruxolitinib Phosphate (Jakafi and Jakavi), the phosphate salt of ruxolitinib which isalso known as INC424, INCB18424 or INCB018424, is a 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 Phosphate (INC-424, INCB-18424, INCB-018424, Jakafi and Jakavi) Chemical Structure CAS No.: 1092939-17-7
Product category: JAK
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
5mg
25mg
50mg
100mg
250mg
500mg
1g
Other Sizes

Other Forms of Ruxolitinib Phosphate (INC-424, INCB-18424, INCB-018424, Jakafi and Jakavi):

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

Purity: ≥98%

Purity: ≥98%

Purity: ≥98%

Purity: ≥98%

Product Description

Ruxolitinib Phosphate (Jakafi and Jakavi), the phosphate salt of ruxolitinib which is also known as INC424, INCB18424 or INCB018424, is a 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, a type of myeloproliferative disorder that affects the bone marrow, and for polycythemia vera (PCV) when there has been an inadequate response to or intolerance of hydroxyurea. It selectively binds to and inhibits protein tyrosine kinases JAK 1 and 2, which may lead to a reduction in inflammation and an inhibition of cellular proliferation.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
Ruxolitinib phosphate (INCB018424) inhibits JAK2V617F-mediated signaling and proliferation in a potent and specific manner. Ruxolitinib phosphate has an EC50 value of 186 nM, which means that it inhibits HEL cell growth. Ruxolitinib phosphate dramatically suppresses the proliferation of hematopoietic progenitor cells and raises Ba/F3-EpoR-JAK2V617F cell apoptosis in primary MPN patient samples [1].
ln Vivo
In mice injected with JAK2V617F-expressing cells, rufolitinib phosphate (180 mg/kg, oral) decreases tumor burden without resulting in anemia or lymphopenia [1].
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]. Fleischman AG, et al. The CSF3R T618I mutation causes a lethal neutrophilic neoplasia in mice that is responsive to therapeutic JAK inhibition. Blood. 2013 Nov 21;122(22):3628-31.
[3]. de Bock CE, et al. HOXA9 Cooperates with Activated JAK/STAT Signaling to Drive Leukemia Development. Cancer Discov. 2018 May;8(5):616-631
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C₁₇H₂₁N₆O₄P
Molecular Weight
404.36
CAS #
1092939-17-7
SMILES
N#CC[C@H](C1CCCC1)N2N=CC(C3=C4C=CNC4=NC=N3)=C2.O=P(O)(O)O
Synonyms
INCB-018424 phosphate, 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: 61 mg/mL (199.1 mM)
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 2.4730 mL 12.3652 mL 24.7304 mL
5 mM 0.4946 mL 2.4730 mL 4.9461 mL
10 mM 0.2473 mL 1.2365 mL 2.4730 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.

Calculator

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What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

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.
             (2) Be sure to add the solvent(s) in order.

Biological Data
  • Ruxolitinib Phosphate

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


    Ruxolitinib Phosphate

  • Ruxolitinib Phosphate

    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 Phosphate

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

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