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Ruxolitinib [941678-49-5]

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Referentie HY-50856-1ml

Formaat : 10mM/1mL

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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. Ruxolitinib induces autophagy and kills tumor cells through toxic mitophagy.

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Ruxolitinib Chemical Structure

CAS No. : 941678-49-5

This product is a controlled substance and not for sale in your territory.

Based on 160 publication(s) in Google Scholar

Other Forms of Ruxolitinib:

Ruxolitinib (S enantiomer) In-stock
Ruxolitinib phosphate In-stock
Deuruxolitinib Obtenir un devis
(Rac)-Ruxolitinib-d₉ Obtenir un devis
Ruxolitinib sulfate Obtenir un devis
Ruxolitinib (Standard) Obtenir un devis

: Ruxolitinib purchased from MedChemExpress. Usage Cited in: Nature. 2022 Sep;609(7928):785-792. [Abstract]; Huh7 cells are pretreated with DMSO, 5 μM Filgotinib, 5 μM Ruxolitinib or 5 μM IFNα-IFNAR-IN-1 hydrochloride for 1 h and infected with MERS-CoV at a MOI of 1. MERS-CoV N gene copy number is quantified by RT-qPCR.

: Ruxolitinib purchased from MedChemExpress. Usage Cited in: Cell Mol Immunol. 2022 Oct;19(10):1130-1140. [Abstract]; The expression of phosphorylated (p-) and unphosphorylated STAT1 and STAT6 in macrophages is assessed by western blotting.

: Ruxolitinib purchased from MedChemExpress. Usage Cited in: Cell Mol Immunol. 2022 Oct;19(10):1130-1140. [Abstract]; Ruxolitinib (100 mg/kg/day; intraperitoneal injection; 8 weeks) reduces the expression of proinflammatory cytokine genes in the livers of ARE-Del+/− mice. RNA is isolated from the livers of Ruxolitinib-treated mice.

: Ruxolitinib purchased from MedChemExpress. Usage Cited in: Cell Mol Immunol. 2022 Oct;19(10):1130-1140. [Abstract]; Levels of IL-6, TNF, and MCP1 production in macrophages isolated from wild-type mice (females/20 weeks) following in vitro treatment with Ruxolitinib are determined utilizing CBA and flow cytometry.

: Ruxolitinib purchased from MedChemExpress. Usage Cited in: Nat Cancer. 2022 Sep;3(9):1071-1087. [Abstract]; Relative cell number of LNCaP/AR cells treated with annotated treatment: 10 µM Enzalutamide (Enz), 5 µM Filgotinib (Filg), 5 µM Ruxolitinib (Ruxo), 1 µM Fludarabine (Flu), 0.2 µM Niclosamide (Nic) and DMSO for 8 days.

: Ruxolitinib purchased from MedChemExpress. Usage Cited in: Theranostics. 2022 Oct 3;12(16):7051-7066.; A549 cells are treated with 2.5 µM BVD and 10 µM Ruxolitinib (Rux) separately or in combination for 2 days. Immunoblotting is conducted to determine pSTAT3-Y705.

: Ruxolitinib purchased from MedChemExpress. Usage Cited in: Proc Natl Acad Sci U S A. 2022 Apr 12;119(15):e2122512119. [Abstract]; Representative DDX4 immunofluorescence following 48 h incubation of ovaries from PND2 mice cultured ex vivo with 1 μM candidate MISR2 agonists Gandotinib, SP600125, CYC-116, Ruxolitinib.

: Ruxolitinib purchased from MedChemExpress. Usage Cited in: Proc Natl Acad Sci U S A. 2022 Apr 12;119(15):e2122512119. [Abstract]; The induction of MIS target genes Id2, Id3, Smad6, and Igfbp5 was recapitulated as measured by qPCR following a 48 h incubation of ex vivo cultured ovaries from PND2 rat with 1 μM candidate MISR2 agonists Gandotinib, SP600125m, CYC-116, Ruxolitinib.

: Ruxolitinib purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2022 May 25;13(5):496. [Abstract]; The xenografts treated with both Trametinib and Ruxolitinib (20 mg/kg; i.p.; every 3 days) show the expression of pSTAT3 and pERK1/2 in xenograft tumors exposed to the indicated treatment. Densitometry analyses of pSTAT3 and pERK1/2 expression normalized to STAT3 and ERK1/2 expression, respectively.

: Ruxolitinib purchased from MedChemExpress. Usage Cited in: J Hematol Oncol. 2021 Jun 24;14(1):97. [Abstract]; Growth curves for DND-41, RPMI-8402 and LOUCY T-ALL cell lines. Growth medium is supplemented with DMSO, MRK-560 100 nM, Ruxolitinib 1 µM or both compounds.

: Ruxolitinib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 Aug 13;12(1):4917. [Abstract]; The A3A mRNA level is monitored in MCF10A cells 16 h after treatment with 3p-hpRNA and JAK inhibitors (JAKi #1: 2 μM Pacritinib, JAKi #2: 2 μM Ruxolitinib).

: Ruxolitinib purchased from MedChemExpress. Usage Cited in: Cancer Commun (Lond). 2021 Dec;41(12):1354-1372. [Abstract]; The MAGE‐C3 overexpressing KYSE30 cells are treated with Ruxolitinib (2 μM, for 20 h.) and probed for STAT1 expression pSTAT1Tyr701. The pSTAT1Tyr701 expression levels are almost unchanged when exposure to Ruxolitinib in presence with IFN‐γ.

: Ruxolitinib purchased from MedChemExpress. Usage Cited in: Cell Rep. 2020 Sep 15;32(11):108158. [Abstract]; Cxcl10 and Ccl5 mRNA levels are analyzed in TNF-α (100 ng/mL)-stimulated BMDMs for 6 h, which are pretreated with notopterol (10 mM) in the presence or absence of ruxolitinib (10 μM) or SD1029 (10 μM) for 3 h.

: Ruxolitinib purchased from MedChemExpress. Usage Cited in: Nat Med. 2018 Aug;24(8):1143-1150. [Abstract]; Immunoblot of pSTAT1, STAT1 and β-actin levels in H69AR cells±200 ng/mL IFNg 10 min pulse followed by 24 h chase in media with DMSO, Ruxolitinib (100 nM) or MRT67307 (1 µM).

: Ruxolitinib purchased from MedChemExpress. Usage Cited in: Cancer Discov. 2018 May;8(5):616-631. [Abstract]; Analysis of PIM1 RNA and protein expression in HOXA9 positive patient derived xenograft (PDX) samples ex vivo after 1 μM Ruxolitinib over 6 hours.

: Ruxolitinib purchased from MedChemExpress. Usage Cited in: Clin Cancer Res. 2018 Apr 15;24(8):1917-1931. [Abstract]; Jak2 is inhibited by lentiviral expression of Jak2 shRNA or control shRNA in CWR22Pc and CWR22Rv1 cells. Alternatively, cells are treated with Jak2 inhibitors AZD1480 (0.8 μM) and Ruxolitinib (0.4 μM) (72 h), followed by Western blot analysis of Jak2 and active Stat5a/b.

: Ruxolitinib purchased from MedChemExpress. Usage Cited in: JCI Insight. 2018 Sep 6;3(17). pii: 120750. [Abstract]; A431 cells are then treated in full growth media with vehicle, CSA (50 ng/mL), Ruxolitinib (20 μM), or both Ruxolitinib and CSA for 36 hours.

: Ruxolitinib purchased from MedChemExpress. Usage Cited in: J Biol Chem. 2015 Nov 27;290(48):29022-34. [Abstract]; 10⁶ autonomous Ba/F3 cells stably transduced with ALL-associated JAK3 mutant V674A or double mutant L857P/Y100A are treated with increasing concentration of Ruxolitinib (0–2 μM). Two hours after treatment, the cells are lysed and subjected to Western blot analysis. Phosphorylation of STAT5, JAK3, and JAK1 is detected using specific anti-pY694 STAT5, anti-pY980/81 JAK3, and anti-pY1034/35 JAK1 antibodies. Membranes are reprobed with anti-STAT5, anti-JAK3, anti-JAK1, and anti-β-actin an

: Ruxolitinib purchased from MedChemExpress. Usage Cited in: Blood. 2013 Nov 21;122(22):3628-31. [Abstract]; Ruxolitinib decreases spleen weight. Mice are sacrificed on day 21 or 24 to evaluate spleen size.

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.

In Vivo

Ruxolitinib (180 mg/kg, orally, twice a day) results in survive rate of greater than 90% by day 22 and markedly reduces splenomegaly and circulating levels of inflammatory cytokines, and preferentially eliminated neoplastic cells, resulting in significantly prolonged survival without myelosuppressive or immunosuppressive effects in a JAK2V617F-driven mouse model^[1].
In the Ruxolitinib group, the primary end point is reached in 41.9% of patients, as compared with 0.7% in the placebo group in the double-blind trial of myelofibrosis. Ruxolitinib results in maintaining of reduction in spleen volume and improvement of 50% or more in the total symptom score^[2].

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

Essai clinique

Masse moléculaire

306.37

Formule

C₁₇H₁₈N₆

CAS No.

941678-49-5

Appearance

Solid

Color

White to light yellow

SMILES

N#CC[C@H](C1CCCC1)N2N=CC(C3=C4C=CNC4=NC=N3)=C2

Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

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.

Calculateur de molarité
Calculateur de dilution

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Pureté et documentation

Purity: 99.99%

Select Batch:

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]

Essai de kinase ^[1]	Recombinant proteins are expressed using Sf21 cells and baculovirus vectors and purified with affinity chromatography. JAK kinase assays use a homogeneous time-resolved fluorescence assay with the peptide substrate (-EQEDEPEGDYFEWLE). Each enzyme reaction is carried out with Ruxolitinib or control, JAK enzyme, 500 nM peptide, adenosine triphosphate (ATP; 1mM), and 2% dimethyl sulfoxide (DMSO) for 1 hour. The 50% inhibitory concentration (IC₅₀) is calculated as INCB018424 concentration required for inhibition of 50% of the fluorescent signal. MCE n'a pas confirmé de manière indépendante l'exactitude de ces méthodes. Ils sont pour référence seulement.
Test cellulaire ^[1]	Cells are seeded at 2×10³/well of white bottom 96-well plates, treated with Ruxolitinib (INCB018424) from DMSO stocks (0.2% final DMSO concentration), and incubated for 48 hours at 37°C with 5% CO₂. Viability is measured by cellular ATP determination using the Cell-Titer Glo luciferase reagent or viable cell counting. Values are transformed to percent inhibition relative to vehicle control, and IC₅₀ curves are fitted according to nonlinear regression analysis of the data using PRISM GraphPad. MCE n'a pas confirmé de manière indépendante l'exactitude de ces méthodes. Ils sont pour référence seulement.
Administration animale ^[1]	Mice are fed standard rodent chow and provided with water ad libitum. Ba/F3-JAK2V617F cells (10⁵ per mouse) are inoculated intravenously into 6- to 8-week-old female BALB/c mice. Survival is monitored daily, and moribund mice are humanely killed and considered deceased at time of death. Treatment with vehicle (5% dimethyl acetamide, 0.5% methocellulose) or Ruxolitinib (INCB018424) begin within 24 hours of cell inoculation, twice daily by oral gavage. Hematologic parameters are measured using a Bayer Advia120 analyzed, and statistical significance is determined using Dunnett testing. MCE n'a pas confirmé de manière indépendante l'exactitude de ces méthodes. Ils sont pour référence seulement.
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]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.2640 mL	16.3201 mL	32.6403 mL	81.6007 mL
	5 mM	0.6528 mL	3.2640 mL	6.5281 mL	16.3201 mL
	10 mM	0.3264 mL	1.6320 mL	3.2640 mL	8.1601 mL
	15 mM	0.2176 mL	1.0880 mL	2.1760 mL	5.4400 mL
	20 mM	0.1632 mL	0.8160 mL	1.6320 mL	4.0800 mL
	25 mM	0.1306 mL	0.6528 mL	1.3056 mL	3.2640 mL
	30 mM	0.1088 mL	0.5440 mL	1.0880 mL	2.7200 mL
	40 mM	0.0816 mL	0.4080 mL	0.8160 mL	2.0400 mL
	50 mM	0.0653 mL	0.3264 mL	0.6528 mL	1.6320 mL
	60 mM	0.0544 mL	0.2720 mL	0.5440 mL	1.3600 mL
	80 mM	0.0408 mL	0.2040 mL	0.4080 mL	1.0200 mL
	100 mM	0.0326 mL	0.1632 mL	0.3264 mL	0.8160 mL

Ruxolitinib Related Classifications

Epigenetics Stem Cell/Wnt Protein Tyrosine Kinase/RTK JAK/STAT Signaling Autophagy Apoptosis
JAK Autophagy Mitophagy Apoptosis

Ruxolitinib [941678-49-5]

Referentie HY-50856-1ml

Neem contact op met een lokale distributeur :

Merk : MedChemExpress

Neem contact op met een lokale distributeur :

Other Forms of Ruxolitinib:

Voir tous les produits spécifiques à Isoform JAK:

Calculateur de molarité

Calculateur de dilution

Complete Stock Solution Preparation Table

Ruxolitinib Related Classifications

Keywords:

Misschien heeft u ook interesse in de volgende producten:

Ruxolitinib [941678-49-5]

Referentie HY-50856-1ml

Neem contact op met een lokale distributeur :

Merk : MedChemExpress

Neem contact op met een lokale distributeur :

Other Forms of Ruxolitinib:

Voir tous les produits spécifiques à Isoform JAK:

Ruxolitinib Related Antibodies

Calculateur de molarité

Calculateur de dilution

Complete Stock Solution Preparation Table

Ruxolitinib Related Classifications

Keywords:

Misschien heeft u ook interesse in de volgende producten: