Ruxolitinib Phosphate
别名: INCB018424, INC424 中文名称：鲁索利替尼,鲁索利替尼磷酸盐
Ruxolitinib Phosphate (INCB018424, INC424)是Ruxolitinib的磷酸盐形式。Ruxolitinib 是第一个应用于临床的，有效的，选择性JAK1/2抑制剂，在无细胞试验中IC50为3.3 nM/2.8 nM。作用于JAK1，JAK2与作用于JAK3相比，选择性高130多倍。Ruxolitinib 通过毒性线粒体自噬杀死肿瘤细胞。Ruxolitinib 可诱导自噬并增强细胞凋亡。
Ruxolitinib Phosphate Chemical Structure
CAS: 1092939-17-7
产品质控
批次：
纯度：
99.99%
99.99
Ruxolitinib Phosphate相关产品
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| 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
| 产品描述 | Ruxolitinib Phosphate (INCB018424, INC424)是Ruxolitinib的磷酸盐形式。Ruxolitinib 是第一个应用于临床的，有效的，选择性JAK1/2抑制剂，在无细胞试验中IC50为3.3 nM/2.8 nM。作用于JAK1，JAK2与作用于JAK3相比，选择性高130多倍。Ruxolitinib 通过毒性线粒体自噬杀死肿瘤细胞。Ruxolitinib 可诱导自噬并增强细胞凋亡。 | ||||
|---|---|---|---|---|---|
| 靶点 |
|
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| 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 | -- |
化学信息&溶解度
| 分子量 | 404.36 | 分子式 | C17H18N6.H3O4P |
| CAS号 | 1092939-17-7 | SDF | -- |
| Smiles | C1CCC(C1)C(CC#N)N2C=C(C=N2)C3=C4C=CNC4=NC=N3.OP(=O)(O)O | ||
| 储存条件(自收到货起) | |||
|
体外溶解度 |
DMSO : 81 mg/mL ( (200.31 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Ethanol : 9 mg/mL (22.25 mM) Water : Insoluble |
摩尔浓度计算器 |
|
体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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