Ruxolitinib (Synonyms: 芦可替尼; INCB18424)

目录号: HY-50856 纯度: 99.90%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

Ruxolitinib (INCB18424) 是具有口服活性的，选择性的 JAK1/2 抑制剂， IC₅₀ 值分别为 3.3 nM 和 2.8 nM，选择性是 JAK3 的 130 多倍。Ruxolitinib 诱导自噬 (autophagy)，通过毒性线粒体自噬 (mitophagy) 杀死肿瘤细胞。

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Ruxolitinib Chemical Structure

CAS No. : 941678-49-5

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥825	In-stock
5 mg	￥750	In-stock
10 mg	￥1100	In-stock
50 mg	￥2800	In-stock
100 mg	￥4500	In-stock
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Customer Review

Other Forms of Ruxolitinib:

MCE 顾客使用本产品发表的 142 篇科研文献

Proliferation Assay

RT-PCR

: Ruxolitinib purchased from MCE. 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 MCE. 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 MCE. 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 MCE. 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 MCE. 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 MCE. 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 MCE. 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 MCE. 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 MCE. 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 MCE. 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 MCE. 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 MCE. 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 MCE. 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 MCE. 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 MCE. 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 MCE. 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 MCE. 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 MCE. 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 MCE. 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.

Ruxolitinib 相关产品

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JAK1 JAK2 JAK3 Tyk2 JAK

生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

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)

细胞效力
(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]

体外研究
(In Vitro)

Ruxolitinib 有效且选择性地抑制 JAK2V617F 介导的信号传导和增殖，以剂量依赖性方式显著增加细胞凋亡，并且在 64 nM 时导致 Ba/F3 细胞中具有去极化线粒体的细胞加倍。
Ruxolitinib 显示出显著的抗红细胞作用集落形成，IC₅₀ 为 67 nM，并抑制正常供体和真性红细胞增多症患者红细胞祖细胞的增殖，IC₅₀ 值分别为 407 nM 和 223 nM^[1]。

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

体内研究
(In Vivo)

Ruxolitinib (180 mg/kg，口服，每天两次) 导致第 22 天时的存活率超过 90%，并显著降低脾肿大和炎症细胞因子的循环水平，并优先消除肿瘤细胞，从而显著延长存活时间，而无骨髓抑制或JAK2V617F 驱动的小鼠模型中的免疫抑制作用^[1]。
在 Ruxolitinib 组中，41.9% 的患者达到主要终点，而安慰剂组为 0.7% 在骨髓纤维化的双盲试验中。Ruxolitinib 可维持脾脏体积减少，总症状评分改善 50% 或更多^[2]。

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

Clinical Trial

分子量

306.37

Formula

C₁₇H₁₈N₆

CAS 号

941678-49-5

性状

固体

颜色

White to light yellow

中文名称

鲁索利替尼；卢索替尼；鲁索替尼；芦可替尼

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

溶解性数据

细胞实验：

DMSO 中的溶解度 : ≥ 100 mg/mL (326.40 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

H₂O 中的溶解度 : < 0.1 mg/mL (insoluble)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	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

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

摩尔计算器
稀释计算器

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

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (6.79 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (6.79 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (6.79 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。

方案一

请依序添加每种溶剂： 0.5% Methylcellulose/saline water
Solubility: 5 mg/mL (16.32 mM); 澄清溶液; 超声助溶
方案二

请依序添加每种溶剂： 5% DMAc in 0.5% Methyl cellulose/Saline water
Solubility: 5 mg/mL (16.32 mM); 悬浊液; 超声助溶

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.99%

选择批次：

Data Sheet (655 KB) SDS (392 KB)

COA (291 KB) HNMR (213 KB) LCMS (336 KB) 元素分析报告 (214 KB)

产品使用指南 (1538 KB)

参考文献

[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]

Kinase Assay ^[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 has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[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 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[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 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[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]

Ruxolitinib 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	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

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Ruxolitinib941678-49-5INCB18424鲁索利替尼卢索替尼鲁索替尼芦可替尼INCB 18424INCB-18424JAKAutophagyMitophagyApoptosisJanus kinaseMitochondrial AutophagyInhibitorinhibitorinhibit

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Ruxolitinib (Synonyms: 芦可替尼; INCB18424)

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MCE 顾客使用本产品发表的 142 篇科研文献

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Ruxolitinib (Synonyms: 芦可替尼; INCB18424)

Customer Review

Other Forms of Ruxolitinib:

Ruxolitinib 相关抗体

MCE 顾客使用本产品发表的 142 篇科研文献

Ruxolitinib 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 JAK 亚型特异性产品:

生物活性

实验参考方法

纯度 & 产品资料

参考文献

Ruxolitinib 相关抗体:

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