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Ruxolitinib [941678-49-5]

Imprimer

Référence HY-50856-5mg

Conditionnement : 5mg

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Description

Ruxolitinib (INCB18424) is an orally active and selective JAK1/2 inhibitor with IC₅₀s of 3.3 nM and 2.8 nM in cell-free assays, and has 130-fold selectivity for JAK1/2 over JAK3^[1]. Ruxolitinib induces autophagy and kills tumor cells through toxic mitophagy^[3].

IC₅₀ & Target^[1]

JAK2

2.8 nM (IC₅₀)

JAK1

3.3 nM (IC₅₀)

Tyk2

19 nM (IC₅₀)

JAK3

428 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	126 nM Compound: 8	Cytotoxicity against mouse BAF3 cells expressing JAK2 V617F mutant after 48 hrs by CellTiterGlo assay Cytotoxicity against mouse BAF3 cells expressing JAK2 V617F mutant after 48 hrs by CellTiterGlo assay	10.1039/C1MD00175B
HCT-116	IC₅₀	> 10 μM Compound: 1	Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay	[PMID: 28953386]
HEL	IC₅₀	> 100 nM Compound: 8	Inhibition of JAK-mediated STAT5 phosphorylation in HEL cells by Western blotting analysis Inhibition of JAK-mediated STAT5 phosphorylation in HEL cells by Western blotting analysis	10.1039/C1MD00175B
HEL	IC₅₀	0.3 μM Compound: 1	Synergistic antiproliferative activity against HEL cells harboring JAK2 V617F mutant assessed as reduction in cell viability after 48 hrs in presence of SAHA by MTT assay Synergistic antiproliferative activity against HEL cells harboring JAK2 V617F mutant assessed as reduction in cell viability after 48 hrs in presence of SAHA by MTT assay	[PMID: 30901208]
HEL	IC₅₀	1.4 μM Compound: INCB018424	Antiproliferative activity against human HEL cells harboring JAK2 V617F mutant assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human HEL cells harboring JAK2 V617F mutant assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 33689932]
HEL	IC₅₀	18.6 μM Compound: 1	Antiproliferative activity against HEL cells harboring JAK2 V617F mutant assessed as reduction in cell viability after 48 hrs by MTT assay Antiproliferative activity against HEL cells harboring JAK2 V617F mutant assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 30901208]
HEL	IC₅₀	2.62 μM Compound: Ruxolitinib	Antiproliferative activity against HEL cells harboring JAK2 V617F mutant after 48 hrs by MTT assay Antiproliferative activity against HEL cells harboring JAK2 V617F mutant after 48 hrs by MTT assay	[PMID: 27774135]
HEL	IC₅₀	7.639 μM Compound: 1	Antiproliferative activity against HEL cells harboring JAK2 V617F mutant measured after 3 days by CCK8 assay Antiproliferative activity against HEL cells harboring JAK2 V617F mutant measured after 3 days by CCK8 assay	[PMID: 30981578]
HEL 92.1.7	IC₅₀	> 4 μM Compound: 1	Antiproliferative activity against human HEL 92.1.7 cells after 36 hrs by PrestoBlue dye based assay Antiproliferative activity against human HEL 92.1.7 cells after 36 hrs by PrestoBlue dye based assay	[PMID: 28953386]
HEL 92.1.7	IC₅₀	> 4 μM Compound: Ruxolitinib	Antiproliferative activity against HEL 92.1.7 cells harboring JAK2 V617F mutant after 36 hrs by PrestoBlue dye based assay Antiproliferative activity against HEL 92.1.7 cells harboring JAK2 V617F mutant after 36 hrs by PrestoBlue dye based assay	[PMID: 27541357]
HEL 92.1.7	IC₅₀	14.7 μM Compound: 1	Antiproliferative activity against HEL 92.1.7 cells assessed as viable cells measured after 3 days by WST-1 assay Antiproliferative activity against HEL 92.1.7 cells assessed as viable cells measured after 3 days by WST-1 assay	[PMID: 27555284]
HEL 92.1.7	IC₅₀	18.06 μM Compound: Ruxolitinib	Cytotoxicity against human HEL 92.1.7 cells expressing JAK2 assessed as reduction in cell viability incubated for 72 hrs by presto blue reagent assay Cytotoxicity against human HEL 92.1.7 cells expressing JAK2 assessed as reduction in cell viability incubated for 72 hrs by presto blue reagent assay	[PMID: 34046625]
Jurkat	IC₅₀	> 5 μM Compound: 1	Antiproliferative activity against human Jurkat cells assessed as reduction in cell viability after 48 hrs by MTT assay Antiproliferative activity against human Jurkat cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 30901208]
K562	IC₅₀	1.03 μM Compound: 1	Synergistic antiproliferative activity against human K562 cells assessed as reduction in cell viability after 48 hrs in presence of SAHA by MTT assay Synergistic antiproliferative activity against human K562 cells assessed as reduction in cell viability after 48 hrs in presence of SAHA by MTT assay	[PMID: 30901208]
K562	IC₅₀	10.3 μM Compound: Ruxolitinib	Antiproliferative activity against human K562 cells after 48 hrs by MTT assay Antiproliferative activity against human K562 cells after 48 hrs by MTT assay	[PMID: 27774135]
K562	IC₅₀	23.2 μM Compound: 1	Antiproliferative activity against human K562 cells assessed as reduction in cell viability after 48 hrs by MTT assay Antiproliferative activity against human K562 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 30901208]
KMS-12-BM	IC₅₀	> 10 μM Compound: 1	Antiproliferative activity against human KMS-12-BM cells after 48 hrs by CellTiter-Glo luminescent assay Antiproliferative activity against human KMS-12-BM cells after 48 hrs by CellTiter-Glo luminescent assay	[PMID: 28953386]
MCF7	IC₅₀	> 10 μM Compound: 1	Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 28953386]
MCF7	IC₅₀	> 5 μM Compound: Ruxolitinib	Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay	[PMID: 27774135]
MDA-MB-231	IC₅₀	> 10 μM Compound: 1	Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay	[PMID: 28953386]
MDA-MB-468	IC₅₀	> 20 μM Compound: INCB018424	Antiproliferative activity against human MDA-MB-468 cells overexpressing STAT3 assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-468 cells overexpressing STAT3 assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 33689932]
MOLM-14	IC₅₀	> 10 μM Compound: 1	Antiproliferative activity against human MOLM14 cells after 48 hrs by CellTiter-Glo luminescent assay Antiproliferative activity against human MOLM14 cells after 48 hrs by CellTiter-Glo luminescent assay	[PMID: 28953386]
MOLT-4	IC₅₀	15.8 μM Compound: 1	Antiproliferative activity against human MOLT4 cells assessed as reduction in cell viability after 48 hrs by MTT assay Antiproliferative activity against human MOLT4 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 30901208]
MOLT-4	IC₅₀	15.8 μM Compound: Ruxolitinib	Antiproliferative activity against human MOLT4 cells after 48 hrs by MTT assay Antiproliferative activity against human MOLT4 cells after 48 hrs by MTT assay	[PMID: 27774135]
MV4-11	IC₅₀	> 10 μM Compound: 1	Antiproliferative activity against human MV4-11 cells after 48 hrs by CellTiter-Glo luminescent assay Antiproliferative activity against human MV4-11 cells after 48 hrs by CellTiter-Glo luminescent assay	[PMID: 28953386]
OPM-2	IC₅₀	> 10 μM Compound: 1	Antiproliferative activity against human OPM2 cells after 48 hrs by CellTiter-Glo luminescent assay Antiproliferative activity against human OPM2 cells after 48 hrs by CellTiter-Glo luminescent assay	[PMID: 28953386]
PBMC	IC₅₀	448 nM Compound: Ruxolitinib	Inhibition IL-7-indcued STAT5 phosphorylation in human PBMC cells by flow cytometry Inhibition IL-7-indcued STAT5 phosphorylation in human PBMC cells by flow cytometry	[PMID: 26927423]
PC-3	IC₅₀	> 10 μM Compound: 1	Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay	[PMID: 28953386]
PC-3	IC₅₀	> 5 μM Compound: Ruxolitinib	Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay	[PMID: 27774135]
Sf21	IC₅₀	0.003 μM Compound: Jakafi	Inhibition of human recombinant JAK2 expressed in Sf21 cells assessed as reduction in Ulight-CAGAGAIETDKEYYTVKD phosphorylation pre-incubated before substrate addition and measured after 60 mins by LANCE detection method Inhibition of human recombinant JAK2 expressed in Sf21 cells assessed as reduction in Ulight-CAGAGAIETDKEYYTVKD phosphorylation pre-incubated before substrate addition and measured after 60 mins by LANCE detection method	[PMID: 27137359]
Sf21	IC₅₀	19 nM Compound: 2, INCB018424	Inhibition of human TYK2 kinase domain expressed in Sf21 cells using EQEDEPEGDYFEWLE as substrate after 1 hr by HTRF assay Inhibition of human TYK2 kinase domain expressed in Sf21 cells using EQEDEPEGDYFEWLE as substrate after 1 hr by HTRF assay	[PMID: 22591402]
Sf21	IC₅₀	2.8 nM Compound: 2, INCB018424	Inhibition of human JAK2 kinase domain expressed in Sf21 cells using EQEDEPEGDYFEWLE as substrate after 1 hr by HTRF assay Inhibition of human JAK2 kinase domain expressed in Sf21 cells using EQEDEPEGDYFEWLE as substrate after 1 hr by HTRF assay	[PMID: 22591402]
Sf21	IC₅₀	2.8 nM Compound: 1	Inhibition of recombinant human N-terminal epitope-tagged JAK2 (828 to 1132 residues) expressed in baculovirus infected Sf21 insect cells using EQEDEPEGDYFEWLE as substrate after 1 hr by homogeneous time-resolved fluorescence assay Inhibition of recombinant human N-terminal epitope-tagged JAK2 (828 to 1132 residues) expressed in baculovirus infected Sf21 insect cells using EQEDEPEGDYFEWLE as substrate after 1 hr by homogeneous time-resolved fluorescence assay	[PMID: 30981578]
Sf21	IC₅₀	3.3 nM Compound: 2, INCB018424	Inhibition of human JAK1 kinase domain expressed in Sf21 cells using EQEDEPEGDYFEWLE as substrate after 1 hr by HTRF assay Inhibition of human JAK1 kinase domain expressed in Sf21 cells using EQEDEPEGDYFEWLE as substrate after 1 hr by HTRF assay	[PMID: 22591402]
Sf21	IC₅₀	4.1 nM Compound: 1	Inhibition of recombinant human C-terminal 6His-tagged JAK2 (808 to end amino acids) expressed in Sf21 cells measured after 1 hr in presence of ATP by TR-FRET assay Inhibition of recombinant human C-terminal 6His-tagged JAK2 (808 to end amino acids) expressed in Sf21 cells measured after 1 hr in presence of ATP by TR-FRET assay	[PMID: 27555284]
Sf21	IC₅₀	428 nM Compound: 2, INCB018424	Inhibition of human JAK3 kinase domain expressed in Sf21 cells using EQEDEPEGDYFEWLE as substrate after 1 hr by HTRF assay Inhibition of human JAK3 kinase domain expressed in Sf21 cells using EQEDEPEGDYFEWLE as substrate after 1 hr by HTRF assay	[PMID: 22591402]
Sf9	IC₅₀	0.0006 μM Compound: 1	Inhibition of human recombinant N-terminal hexahistidine tagged JAK2 JH1 catalytic domain (835 to 1132 residues) expressed in baculovirus infected Sf9 cells using Tyr6 peptide as substrate incubated for 30 secs under shaking condition measured after 1 hr Inhibition of human recombinant N-terminal hexahistidine tagged JAK2 JH1 catalytic domain (835 to 1132 residues) expressed in baculovirus infected Sf9 cells using Tyr6 peptide as substrate incubated for 30 secs under shaking condition measured after 1 hr	[PMID: 30981578]
Sf9	IC₅₀	0.004 μM Compound: 1	Inhibition of human recombinant N-terminal hexahistidine tagged JAK1 JH1 catalytic domain (854 to 1154 residues) expressed in baculovirus infected Sf9 cells using Tyr6 peptide as substrate incubated for 30 secs under shaking condition measured after 1 hr Inhibition of human recombinant N-terminal hexahistidine tagged JAK1 JH1 catalytic domain (854 to 1154 residues) expressed in baculovirus infected Sf9 cells using Tyr6 peptide as substrate incubated for 30 secs under shaking condition measured after 1 hr	[PMID: 30981578]
Sf9	IC₅₀	0.051 μM Compound: 1	Inhibition of human recombinant C-terminal hexahistidine tagged JAK3 JH1 catalytic domain (811 to 1124 residues) expressed in baculovirus infected Sf9 cells using Tyr6 peptide as substrate incubated for 30 secs under shaking condition measured after 1 hr Inhibition of human recombinant C-terminal hexahistidine tagged JAK3 JH1 catalytic domain (811 to 1124 residues) expressed in baculovirus infected Sf9 cells using Tyr6 peptide as substrate incubated for 30 secs under shaking condition measured after 1 hr	[PMID: 30981578]
Sf9	IC₅₀	2.8 nM Compound: 1	Inhibition of human JAK2 (828 to 1132 residues) expressed in baculovirus infected Sf9 insect cells using EQEDEPEGDYFEWLE as substrate after 1 hr by fluorescence assay Inhibition of human JAK2 (828 to 1132 residues) expressed in baculovirus infected Sf9 insect cells using EQEDEPEGDYFEWLE as substrate after 1 hr by fluorescence assay	[PMID: 30833158]
Sf9	IC₅₀	3.3 nM Compound: 1	Inhibition of human JAK1 (837 to 1142 residues) expressed in baculovirus infected Sf9 insect cells using EQEDEPEGDYFEWLE as substrate after 1 hr by fluorescence assay Inhibition of human JAK1 (837 to 1142 residues) expressed in baculovirus infected Sf9 insect cells using EQEDEPEGDYFEWLE as substrate after 1 hr by fluorescence assay	[PMID: 30833158]
TF-1	EC₅₀	12 nM Compound: 2, INCB018424	Inhibition of JAK2 in human TF1 cells assessed as inhibition of EPO-induced STAT5 phosphorylation incubated for 20 mins prior to EPO-induction measured after 30 to 45 mins Inhibition of JAK2 in human TF1 cells assessed as inhibition of EPO-induced STAT5 phosphorylation incubated for 20 mins prior to EPO-induction measured after 30 to 45 mins	[PMID: 22698084]
TF-1	IC₅₀	14.35 μM Compound: Ruxolitinib	Cytotoxicity against human TF-1 cells expressing JAK2 assessed as reduction in cell viability incubated for 72 hrs by presto blue reagent assay Cytotoxicity against human TF-1 cells expressing JAK2 assessed as reduction in cell viability incubated for 72 hrs by presto blue reagent assay	[PMID: 34046625]
TF-1	EC₅₀	24 nM Compound: 2, INCB018424	Inhibition of JAK1 in human TF1 cells assessed as inhibition of IL6-induced STAT3 phosphorylation incubated for 20 mins prior to IL6-induction measured after 30 to 45 mins Inhibition of JAK1 in human TF1 cells assessed as inhibition of IL6-induced STAT3 phosphorylation incubated for 20 mins prior to IL6-induction measured after 30 to 45 mins	[PMID: 22698084]
TF-1	IC₅₀	6.85 nM Compound: Ruxolitinib	Inhibition of JAK2 in human TF1 cells assessed as reduction in STAT5 phosphorylation incubated for 30 mins in presence of human recombinant EPO Inhibition of JAK2 in human TF1 cells assessed as reduction in STAT5 phosphorylation incubated for 30 mins in presence of human recombinant EPO	[PMID: 23061660]
Vero	IC₅₀	> 50 μM Compound: Ruxolitinib	Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability incubated for 72 hrs by presto blue reagent assay Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability incubated for 72 hrs by presto blue reagent assay	[PMID: 34046625]

In Vitro

Ruxolitinib potently and selectively inhibits JAK2V617F-mediated signaling and proliferation, markedly increases apoptosis in a dose dependent manner, and at 64 nM results in a doubling of cells with depolarized mitochondria in Ba/F3 cells.
Ruxolitinib demonstrates remarkable potency against erythroid colony formation with IC₅₀ of 67 nM, and inhibits proliferating of erythroid progenitors from normal donors and polycythemia vera patients with IC₅₀ values of 407 nM and 223 nM, respectively^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Solvant et solubilité

In Vitro:

DMSO : ≥ 100 mg/mL (326.40 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (6.79 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (6.79 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (6.79 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 0.5% Methylcellulose/saline water
Solubility: 5 mg/mL (16.32 mM); Clear solution; Need ultrasonic
Protocol 2

Add each solvent one by one: 5% DMAc in 0.5% Methyl cellulose/Saline water
Solubility: 5 mg/mL (16.32 mM); Suspended solution; Need ultrasonic

Pureté et documentation

Purity: 99.99%

Fiche technique (283 KB) SDS (392 KB)

COA (254 KB) HNMR (213 KB) LCMS (336 KB) Elemental Analysis Report (111 KB)

Instruction de manipulation (2659 KB)

Références

[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. [Content Brief]

[2]. Verstovsek S, et al. A double-blind, placebo-controlled trial of ruxolitinib for myelofibrosis. N Engl J Med, 2012, 366(9), 799-807. [Content Brief]

[3]. Tavallai M, et al. Rationally Repurposing Ruxolitinib (Jakafi (®)) as a Solid Tumor Therapeutic.Front Oncol. 2016 Jun 13;6:142. [Content Brief]

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Ruxolitinib [941678-49-5]

Référence HY-50856-5mg

Contactez votre distributeur local :

Marque : MedChemExpress

Contactez votre distributeur local :

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