Ruxolitinib (INCB-018424; INC-424)

Alias: INCB-018424, INCB 018424, INCB 18424, INCB-18424; INCB018424; INC424, INC424, INC-424; INCB18424, Jakafi and Jakavi (trade name)
Cat No.:V0314 Purity: ≥98%
Ruxolitinib (formerly INC424, INCB18424, INCB018424; trade name Jakafi and Jakavi) is the first-in class, potent, selective, and orally bioavailabe 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 (INCB-018424; INC-424) Chemical Structure CAS No.: 941678-49-5
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
10mg
25mg
50mg
100mg
250mg
500mg
1g
Other Sizes

Other Forms of Ruxolitinib (INCB-018424; INC-424):

  • S-Ruxolitinib (INCB-018424)
  • Ruxolitinib Phosphate (INC-424, INCB-18424, INCB-018424, Jakafi and Jakavi)
  • (Rac)-Ruxolitinib-d9 ((Rac)-INCB18424-d9; Ruxotinib racemate-d9)
  • Deuruxolitinib (CTP-543)
  • 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%

Product Description

Ruxolitinib (formerly INC424, INCB18424, INCB018424; trade name Jakafi and Jakavi) is the first-in class, potent, selective, and orally bioavailabe 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 produces a dose-dependent increase in apoptosis, a doubling of cells with depolarized mitochondria in Ba/F3 cells, and a powerful and specific inhibition of JAK2V617F-mediated signaling and proliferation. Ruxolitinib reduced the proliferation of erythroid progenitor cells from normal donors and polycythemia vera patients with IC50 values of 407 nM and 223 nM, respectively, and demonstrated substantial anti-erythroid colony formation with an IC50 of 67 nM [1].
ln Vivo
In JAK2V617F-driven mouse models, rufolitinib (180 mg/kg, PO, twice daily) did not cause myelosuppression or immunosuppression, but it did significantly prolong survival by reducing splenomegaly and circulating levels of inflammatory cytokines and preferentially eliminating tumor cells. At day 22, survival rates were above 90% [1]. In the myelofibrosis double-blind trial, 41.9% of patients in the ruxolitinib group and 0.7% of patients in the placebo group achieved the primary endpoint. Ruxolitinib improves overall symptom scores by 50% or more while maintaining spleen volume reduction [2].
Animal Protocol
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]. Tavallai M, et al. Rationally Repurposing Ruxolitinib (Jakafi (®)) as a Solid Tumor Therapeutic.Front Oncol. 2016 Jun 13;6:14
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C17H18N6
Molecular Weight
306.3650
CAS #
941678-49-5
SMILES
N#CC[C@@H](N1N=CC(C2=C3C(NC=C3)=NC=N2)=C1)C4CCCC4
Chemical Name
(R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile
Synonyms
INCB-018424, INCB 018424, INCB 18424, INCB-18424; INCB018424; INC424, INC424, INC-424; INCB18424, 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 3.2640 mL 16.3201 mL 32.6403 mL
5 mM 0.6528 mL 3.2640 mL 6.5281 mL
10 mM 0.3264 mL 1.6320 mL 3.2640 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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An example of molarity calculation using the molarity calculator is shown below:
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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What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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g/mol

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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Definitions of molecular mass, molecular weight, molar mass and molar weight:
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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 (INCB018424)

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


    Ruxolitinib (INCB018424)

  • Ruxolitinib (INCB018424)

    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 (INCB018424)

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

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