Ruxolitinib Phosphate

別名：INCB018424, INC424

製品コード：S5243 純度：99.99%

Ruxolitinib Phosphate (INCB018424, INC424) is the phosphate salt form of Ruxolitinib. Ruxolitinib is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM in cell-free assays, >130-fold selectivity for JAK1/2 versus JAK3. Ruxolitinib kills tumor cells through toxic mitophagy. Ruxolitinib induces autophagy and enhances apoptosis.

CAS No. 1092939-17-7

サイズ	価格(税別)	在庫状況
25mg	JPY 22000	国内在庫あり
100mg	JPY 55500	国内在庫あり
1g	JPY 190500	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（180）

製品安全説明書

現在のバッチを見る：純度： 99.99%

99.99

Ruxolitinib Phosphate関連製品

関連ターゲット	JAK1 JAK2 JAK3 Tyk2	もっと見る
関連製品	AZD1480 WP1066 Momelotinib (CYT387) Filgotinib (GLPG0634) AT9283 Gandotinib (LY2784544) TG101209 Cerdulatinib (PRT062070) hydrochloride Pacritinib NVP-BSK805 2HCl WHI-P154 FLLL32 Decernotinib (VX-509) CEP-33779 AZ 960 Cerdulatinib (PRT062070) ZM 39923 HCl XL019 BMS-911543 Curcumol Solcitinib Oclacitinib maleate Pyridone 6 Creatine Ritlecitinib (PF-06651600) Deucravacitinib (BMS-986165) Itacitinib (INCB39110) Peficitinib BD750 WHI-P97 JANEX-1 Brevilin A 1,2,3,4,5,6-Hexabromocyclohexane Brepocitinib (PF-06700841) FM-381 SAR-20347 Selective JAK3 inhibitor 1	もっと見る
関連化合物ライブラリー	Kinase Inhibitor Library FDA-approved Drug Library Natural Product Library Tyrosine Kinase Inhibitor Library JAK/STAT compound library	もっと見る

シグナル伝達経路

JAKシグナル伝達経路

JAK阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
TALL-1	Function assay	1 uM	3 hrs	Inhibition of JAK3 in human TALL-1 cells assessed as inhibition of IL-2 induced STAT5 phosphorylation at 1 uM preincubated for 3 hrs followed by IL-2 induction measured after 30 mins by immunoblotting	26258521
OCL-AML5	Function assay	1 uM	3 hrs	Inhibition of JAK2 in human OCL-AML5 cells assessed as inhibition of GM-CSF induced STAT5 phosphorylation at 1 uM preincubated for 3 hrs followed by GM-CSF induction measured after 30 mins by immunoblotting	26258521
HCC827	Function assay	30 uM	24 hrs	Inhibition of JAK2 in human gefitinib-resistant HCC827 cells assessed as inhibition of STAT3 phosphorylation at Y705 site at 30 uM measured after 24 hrs by western blotting analysis	27555284
HCC827	Function assay	30 uM	24 hrs	Inhibition of JAK2 in wild-type human HCC827 cells assessed as inhibition of STAT3 phosphorylation at Y705 site at 30 uM measured after 24 hrs by western blotting analysis	27555284
HeLa	Function assay	0.1 to 1 uM	1 hr	Inhibition of JAK2 in human HeLa cells assessed as reduction in STAT5 phosphorylation at 0.1 to 1 uM after 1 hr by immunoblot analysis	30243158
HeLa	Function assay	0.1 to 1 uM	1 hr	Inhibition of JAK2 in human HeLa cells assessed as increase in JAK2 phosphorylation at 0.1 to 1 uM after 1 hr by immunoblot analysis	30243158
A549	Function assay	80 to 400 nM	6 hrs	Inhibition of HDAC2 in human A549 cells assessed as increase in acetyl histone H4 level at 80 to 400 nM after 6 hrs by Western blot analysis	30901208
A549	Function assay	80 to 400 nM	6 hrs	Inhibition of HDAC1 in human A549 cells assessed as increase in acetyl histone H4 level at 80 to 400 nM after 6 hrs by Western blot analysis	30901208
A549	Function assay	80 to 400 nM	6 hrs	Inhibition of HDAC3 in human A549 cells assessed as increase in acetyl histone H4 level at 80 to 400 nM after 6 hrs by Western blot analysis	30901208
A549	Function assay	80 to 400 nM	6 hrs	Inhibition of HDAC6 in human A549 cells assessed as increase in acetyl alpha tubulin level at 80 to 400 nM after 6 hrs by Western blot analysis	30901208
HEL	Function assay	100 mg/kg	5 days	Drug level in tumor of BALB/c nu mouse xenografted with HEL cells at 100 mg/kg/day, ip administered for 5 days and measured 1 hr post-last dose by LC-MS/MS analysis	30901208
Sf21	Function assay		1 hr	Inhibition of human JAK2 kinase domain expressed in Sf21 cells using EQEDEPEGDYFEWLE as substrate after 1 hr by HTRF assay, IC50=0.0028μM	22591402
Sf21	Function assay		1 hr	Inhibition of human JAK1 kinase domain expressed in Sf21 cells using EQEDEPEGDYFEWLE as substrate after 1 hr by HTRF assay, IC50=0.0033μM	22591402
Sf21	Function assay		1 hr	Inhibition of human TYK2 kinase domain expressed in Sf21 cells using EQEDEPEGDYFEWLE as substrate after 1 hr by HTRF assay, IC50=0.019μM	22591402
Sf21	Function assay		1 hr	Inhibition of human JAK3 kinase domain expressed in Sf21 cells using EQEDEPEGDYFEWLE as substrate after 1 hr by HTRF assay, IC50=0.428μM	22591402
TF1	Function assay		20 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, EC50=0.012μM	22698084
TF1	Function assay		20 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, EC50=0.024μM	22698084
TF1	Function assay		30 mins	Inhibition of JAK2 in human TF1 cells assessed as reduction in STAT5 phosphorylation incubated for 30 mins in presence of human recombinant EPO, IC50=0.00685μM	23061660
Sf9	Function assay		1 hr	Inhibition of human JAK2 (828-1132) expressed in baculovirus-infected Sf9 cells using EQEDEPEGDYFEWLE as substrate after 1 hr by HTRF assay, Ki=0.0001μM	23668484
Sf9	Function assay		1 hr	Inhibition of human JAK1 (837-1142) expressed in baculovirus-infected Sf9 cells using EQEDEPEGDYFEWLE as substrate after 1 hr by HTRF assay, Ki=0.0002μM	23668484
Sf9	Function assay		1 hr	Inhibition of human TYK2 (873-1187) expressed in baculovirus-infected Sf9 cells using EQEDEPEGDYFEWLE as substrate after 1 hr by HTRF assay, Ki=0.0005μM	23668484
Sf9	Function assay		1 hr	Inhibition of human JAK3 (781-1124) expressed in baculovirus-infected Sf9 cells using EQEDEPEGDYFEWLE as substrate after 1 hr by HTRF assay, Ki=0.0032μM	23668484
CD34+	Function assay		45 mins	Inhibition of JAK2 homodimer in human CD34+ cells spiked into human whole blood assessed as inhibition of EPO-induced STAT-5 phosphorylation preincubated for 45 mins followed by EPO addition measured after 15 mins by FACS analysis, IC50=0.677μM	24417533
BA/F3	Antiproliferative assay		72 hrs	Antiproliferative activity against mouse BA/F3 cells expressing TEL-JAK1 after 72 hrs by cell titer glo assay	26258521
BA/F3	Antiproliferative assay		72 hrs	Antiproliferative activity against mouse BA/F3 cells expressing TEL-JAK2 after 72 hrs by cell titer glo assay	26258521
Sf21	Function assay		60 mins	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, IC50=0.003μM	27137359
Sf21	Function assay		1 hr	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, IC50=0.0041μM	27555284
HEL 92.1.7	Antiproliferative assay		3 days	Antiproliferative activity against HEL 92.1.7 cells assessed as viable cells measured after 3 days by WST-1 assay, IC50=14.7μM	27555284
HEL	Antiproliferative assay		48 hrs	Antiproliferative activity against HEL cells harboring JAK2 V617F mutant after 48 hrs by MTT assay, IC50=2.62μM	27774135
K562	Antiproliferative assay		48 hrs	Antiproliferative activity against human K562 cells after 48 hrs by MTT assay, IC50=10.3μM	27774135
MOLT4	Antiproliferative assay		48 hrs	Antiproliferative activity against human MOLT4 cells after 48 hrs by MTT assay, IC50=15.8μM	27774135
Sf9	Function assay		1 hr	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, IC50=0.0028μM	30833158
Sf9	Function assay		1 hr	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, IC50=0.0033μM	30833158
HEL	Antiproliferative assay		48 hrs	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, IC50=0.3μM	30901208
K562	Antiproliferative assay		48 hrs	Synergistic antiproliferative activity against human K562 cells assessed as reduction in cell viability after 48 hrs in presence of SAHA by MTT assay, IC50=1.03μM	30901208
MOLT4	Antiproliferative assay		48 hrs	Antiproliferative activity against human MOLT4 cells assessed as reduction in cell viability after 48 hrs by MTT assay, IC50=15.8μM	30901208
HEL	Antiproliferative assay		48 hrs	Antiproliferative activity against HEL cells harboring JAK2 V617F mutant assessed as reduction in cell viability after 48 hrs by MTT assay, IC50=18.6μM	30901208
K562	Antiproliferative assay		48 hrs	Antiproliferative activity against human K562 cells assessed as reduction in cell viability after 48 hrs by MTT assay, IC50=23.2μM	30901208
Sf9	Function assay		30 secs	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 , IC50=0.0006μM	30981578
Sf21	Function assay		1 hr	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, IC50=0.0028μM	30981578
Sf9	Function assay		30 secs	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 , IC50=0.004μM	30981578
Sf9	Function assay		30 secs	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 , IC50=0.051μM	30981578
HEL	Antiproliferative assay		3 days	Antiproliferative activity against HEL cells harboring JAK2 V617F mutant measured after 3 days by CCK8 assay, IC50=7.639μM	30981578
insect cells	Function assay		10 mins	Inhibition of recombinant human N-terminal GST-tagged JAK1 (866 to 1154 residues) expressed in insect cells using FITC-labeled C6-KKHTDDGYMPMSPGVA-NH peptide as substrate after 10 mins in presence of 5 mM ATP by caliper mobility shift assay, IC50=0.02μM	32297743
insect cells	Function assay		10 mins	Inhibition of recombinant human N-terminal GST-tagged JAK2 (831 to 1132 residues) expressed in insect cells using 5FAM-labeled GEEPLYWSFPAKKK-NH2 peptide as substrate after 10 mins in presence of 5 mM ATP by caliper mobility shift assay, IC50=0.02μM	32297743
BAF3	Cytotoxicity assay		48 hrs	Cytotoxicity against mouse BAF3 cells expressing JAK2 V617F mutant after 48 hrs by CellTiterGlo assay, IC50=0.126μM	ChEMBL
SET2	Function assay			Inhibition of JAK2 V617F mutant in human SET2 cells assessed as reduction in STAT5 phosphorylation, IC50=0.00184μM	23061660
T-cells	Function assay			Inhibition of JAK3/1 in human T cells expressing CD3 assessed as inhibition of IL2-stimulated STAT5a phosphorylation, IC50=0.023μM	23540648
T-cells	Function assay			Inhibition of JAK2/1 in human T cells expressing CD3 assessed as inhibition of IFNgamma-stimulated STAT1 phosphorylation, IC50=0.031μM	23540648
CD34+	Function assay			Inhibition of JAK2 in human CD34+ cells assessed as inhibition of EPO-mediated cell proliferation, IC50=0.008μM	26927423
PBMC	Function assay			Inhibition of JAK1 in human PBMC cells assessed as inhibition of IL-6-induced MCP1 secretion, IC50=0.04μM	26927423
PBMC	Function assay			Inhibition IL-7-indcued STAT5 phosphorylation in human PBMC cells by flow cytometry, IC50=0.448μM	26927423
BaF3	Function assay			Inhibition of JAK2 V617F mutant expressed in mouse BaF3 cells cells assessed as reduction in cell viability, EC50=0.186μM	27555284
NCI-H23	Antiproliferative assay			Antiproliferative activity against human NCI-H23 cells harboring KRAS G12C mutant at	28038940
NCI-H358	Antiproliferative assay			Antiproliferative activity against human NCI-H358 cells harboring KRAS G12C mutant at	28038940
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
NB1643	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
Sf9	Function assay			Binding affinity to human recombinant N-terminal hexahistidine tagged JAK2 JH1 catalytic domain (835 to 1132 residues) expressed in baculovirus infected Sf9 cells assessed as dissociation constant by surface plasmon resonance assay, Kd=0.0282μM	30981578
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生物活性

製品説明

Targets

JAK2 ^[1] (Cell-free assay)	JAK1 ^[1] (Cell-free assay)
2.8 nM	3.3 nM

In Vitro
In vitro	INCB018424 potently and selectively inhibits JAK2V617F-mediated signaling and proliferation in Ba/F3 cells and HEL cells. INCB018424 markedly increases apoptosis in a dose dependent manner in Ba/F3 cells. INCB018424 (64 nM) results in a doubling of cells with depolarized mitochondria in Ba/F3 cells. INCB018424 inhibits proliferating of erythroid progenitors from normal donors and polycythemia vera patients with IC50 of 407 nM and 223 nM, respectively. INCB018424 demonstrates remarkable potency against erythroid colony formation with IC50 of 67nM. ^[1]
Kinase Assay	Binding assay
Kinase Assay	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.
細胞実験	細胞株	Ba/F3 and HEL cells
	濃度	3 μM
	反応時間	48 h
	実験の流れ	Cells are seeded at 2 × 10³/well of white bottom 96-well plates, treated with INCB018424 from DMSO stocks (0.2% final DMSO concentration), and incubated for 48 hours at 37 ℃ 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.

In Vivo
In Vivo	INCB018424 (180 mg/kg, orally, twice a day) results in survive rate of greater than 90% by day 22 in a JAK2V617F-driven mouse model. INCB018424 (180 mg/kg, orally, twice a day) 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] The primary end point is reached in 41.9% of patients in the Ruxolitinib group 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] A total of 28% of the patients in the Ruxolitinib (15 mg twice daily) group has at least a 35% reduction in spleen volume at week 48 in patients with myelofibrosis, as compared with 0% in the group receiving the best available therapy. The mean palpable spleen length has decreased by 56% with Ruxolitinib but has increased by 4% with the best available therapy at week 48. Patients in the ruxolitinib group has an improvement in overall quality-of-life measures and a reduction in symptoms associated with myelofibrosis. ^[3]
動物実験	動物モデル	JAK2V617F-driven mouse model
	投与量	180 mg/kg
	投与経路	o.g.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT06310304	Active not recruiting	Healthy Participants	Incyte Corporation	March 26 2024	Phase 1
NCT02596347	Completed	Chronic Beryllium Disease (CBD)\|Beryllium Sensitization (BeS)	National Jewish Health	April 2015	--

参考
[1] Quintas-Cardama A, et al. Blood, 2010, 115(15), 3109-3117. [2] Verstovsek S, et al. N Engl J Med, 2012, 366(9), 799-807. [3] Harrison C, et al. N Engl J Med, 2012, 366(9), 787-798. [4] Alfonso Quintás-Cardama, et al. Blood . 2010 Apr 15;115(15):3109-17. + 展開

参考

[4] Alfonso Quintás-Cardama, et al. Blood . 2010 Apr 15;115(15):3109-17.

+ 展開

化学情報

分子量	404.36	化学式	C₁₇H₁₈N₆.H₃O₄P
CAS No.	1092939-17-7	SDF	--
Smiles	C1CCC(C1)C(CC#N)N2C=C(C=N2)C3=C4C=CNC4=NC=N3.OP(=O)(O)O
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1个月-20°Cin solvent

In vitro
Batch:

DMSO : 81 mg/mL ( (200.31 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Ethanol : 9 mg/mL

Water : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):