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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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1g |
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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 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.
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].
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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].
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Animal Protocol |
JAK2V617F-driven mouse model;
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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 |
Molecular Formula |
C17H18N6
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Molecular Weight |
306.3650
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CAS # |
941678-49-5
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Related CAS # |
Ruxolitinib (S enantiomer);941685-37-6;Ruxolitinib phosphate;1092939-17-7;(Rac)-Ruxolitinib-d9;2469553-67-9;Deuruxolitinib-d8;1513883-39-0;Ruxolitinib sulfate;1092939-16-6
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SMILES |
N#CC[C@@H](N1N=CC(C2=C3C(NC=C3)=NC=N2)=C1)C4CCCC4
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Chemical Name |
(R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile
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Synonyms |
INCB-018424, INCB 018424, INCB 18424, INCB-18424; INCB018424; INC424, INC424, INC-424; INCB18424, Jakafi and Jakavi (trade name)
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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)
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Solubility (In Vitro) |
DMSO: 61 mg/mL (199.1 mM)
Water:<1 mg/mL
Ethanol:<1 mg/mL
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Solubility (In Vivo) |
Solubility in Formulation 1: 5 mg/mL (16.32 mM) in 5% DMAC in 0.5% methylcellulose aqueous solution (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
Solubility in Formulation 2: ≥ 2.08 mg/mL (6.79 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (6.79 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 2.08 mg/mL (6.79 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL corn oil and mix evenly. Solubility in Formulation 5: 2% DMSO+30% PEG 300+ddH2O:5mg/mL Solubility in Formulation 6: 5 mg/mL (16.32 mM) in 0.5% Methylcellulose/saline water (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. |
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.
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.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT06213831 | Recruiting | Drug: Ruxolitinib Cream 1.5% | Prurigo Nodularis | Incyte Corporation | February 27, 2024 | Phase 1 |
NCT06310304 | Active, not recruiting NEW |
Drug: Ruxolitinib IR Drug: Ruxolitinib XR |
Healthy Participants | Incyte Corporation | March 26, 2024 | Phase 1 |
NCT05034822 | Completed | Drug: Ruxolitinib cream | Atopic Dermatitis | Incyte Corporation | December 16, 2021 | Phase 1 |
NCT05456529 | Active, not recruiting | Drug: Ruxolitinib Cream | Atopic Dermatitis (AD) | Incyte Corporation | September 1, 2022 | Phase 3 |
INCB018424 (Ruxolitinib)treatment improves viability and splenomegaly in a JAK2V617F-driven model of malignant disease.Blood.2010 Apr 15;115(15):3109-17. |
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. td> |
INCB018424 does not affect normal hematologic parameters.Blood.2010 Apr 15;115(15):3109-17. td> |