Ruxolitinib Phosphate

別名: INCB018424, INC424 中文名稱：魯索利替尼,魯索利替尼磷酸鹽

目錄號(hào)：S5243 Purity: 99.99%

Ruxolitinib Phosphate (INCB018424, INC424)是Ruxolitinib的磷酸鹽形式。Ruxolitinib 是第一個(gè)應(yīng)用于臨床的，有效的，選擇性JAK1/2抑制劑，在無(wú)細(xì)胞試驗(yàn)中IC50為3.3 nM/2.8 nM。作用于JAK1，JAK2與作用于JAK3相比，選擇性高130多倍。Ruxolitinib 通過(guò)毒性線粒體自噬殺死腫瘤細(xì)胞。Ruxolitinib 可誘導(dǎo)自噬并增強(qiáng)細(xì)胞凋亡。

Ruxolitinib Phosphate Chemical Structure

CAS: 1092939-17-7

規(guī)格	價(jià)格	庫(kù)存
10mM (1mL in DMSO)	1040.13	現(xiàn)貨
25mg	876.5	現(xiàn)貨
100mg	3030.5	現(xiàn)貨
1g	10401.3	現(xiàn)貨
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產(chǎn)品質(zhì)控

批次：純度： 99.99%

99.99

Ruxolitinib Phosphate相關(guān)產(chǎn)品

相關(guān)靶點(diǎn)	JAK1 JAK2 JAK3 Tyk2	點(diǎn)擊展開(kāi)
相關(guān)產(chǎn)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	點(diǎn)擊展開(kāi)
相關(guān)化合物庫(kù)	激酶抑制劑庫(kù) FDA藥物庫(kù) 天然產(chǎn)物庫(kù) 酪氨酸激酶抑制劑分子庫(kù) JAK-STAT信號(hào)通路庫(kù)	點(diǎn)擊展開(kāi)

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系	實(shí)驗(yàn)類型	給藥濃度	孵育時(shí)間	活性描述	文獻(xiàn)信息
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

產(chǎn)品描述

靶點(diǎn)

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

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試驗(yàn)信息 (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	--

參考文獻(xiàn)
[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(kāi)

參考文獻(xiàn)

[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(kāi)

化學(xué)信息&溶解度

分子量	404.36	分子式	C₁₇H₁₈N₆.H₃O₄P
CAS號(hào)	1092939-17-7	SDF	--
Smiles	C1CCC(C1)C(CC#N)N2C=C(C=N2)C3=C4C=CNC4=NC=N3.OP(=O)(O)O
儲(chǔ)存條件(自收到貨起)	3年-20°C粉狀	儲(chǔ)備液保存和期限建議分裝儲(chǔ)備液，避免反復(fù)凍融！	1年-80°C溶于溶劑
儲(chǔ)存條件(自收到貨起)	3年-20°C粉狀	儲(chǔ)備液保存和期限建議分裝儲(chǔ)備液，避免反復(fù)凍融！	1個(gè)月-20°C溶于溶劑

體外溶解度
批次：

DMSO : 81 mg/mL ( (200.31 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開(kāi)封DMSO)

Ethanol : 9 mg/mL (22.25 mM)

Water : Insoluble

DMSO : 81 mg/mL ( (200.31 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開(kāi)封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 81 mg/mL ( (200.31 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開(kāi)封DMSO)

Ethanol : 6 mg/mL (14.83 mM)

Water : Insoluble

DMSO : 80 mg/mL ( (197.84 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開(kāi)封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 80 mg/mL ( (197.84 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開(kāi)封DMSO)

Water : 20 mg/mL (49.46 mM)

Ethanol : 8 mg/mL (19.78 mM)

摩爾濃度計(jì)算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請(qǐng)按從左到右的順序依次添加，澄清后再加入下一溶劑

動(dòng)物體內(nèi)配方計(jì)算器

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量	濃度	體積	分子量
=	×	×

稀釋計(jì)算器分子量計(jì)算器

動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過(guò)程中的損耗，建議多配一只動(dòng)物的藥量）

給藥劑量 mg/kg 動(dòng)物平均體重 g 每只動(dòng)物給藥體積 μL 動(dòng)物數(shù)量只

第二步：請(qǐng)輸入動(dòng)物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

計(jì)算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過(guò)該批次藥物DMSO溶解度，請(qǐng)先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH₂O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

技術(shù)支持

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操作手冊(cè)

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* 必填項(xiàng)

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):

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Ruxolitinib Phosphate

產(chǎn)品質(zhì)控

Ruxolitinib Phosphate相關(guān)產(chǎn)品

相關(guān)信號(hào)通路圖

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

生物活性

化學(xué)信息&溶解度

實(shí)驗(yàn)計(jì)算

技術(shù)支持