磷酸鲁索利替尼 T3043

Product Introduction
Bioactivity


英文名: Ruxolitinib phosphate

描述: Ruxolitinib phosphate (INCB018424) 是一种 JAK1/2抑制剂，IC50分别为3.3 nM/2.8 nM，对 JAK1/2 的选择性是 JAK3 的 130 倍以上。

细胞实验: Ruxolitinib phosphate is dissolved in 0.2% DMSO. Cells are seeded at 2000/well of white bottom 96-well plates, treated with compounds 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.

体外活性: Ruxolitinib (INCB018424) potently and selectively inhibits JAK2V617F-mediated signaling and proliferation. Ruxolitinib inhibits the growth of HEL cells with EC50 of 186 nM. Ruxolitinib markedly increases apoptosis in Ba/F3-EpoR-JAK2V617F cell system. It also inhibits hematopoietic progenitor cell proliferation in primary MPN patient samples[1].

体内活性: Ruxolitinib (180 mg/kg, p.o.) reduces the tumor burden of mice inoculated with JAK2V617F-expressing cells while not causing anemia or lymphopenia[1].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 50 mg/mL (123.65 mM)
H2O : 8 mg/mL(19.8 mM)


关键字: Ruxolitinib | inhibit | INCB 018424 Phosphate | Mitophagy | INCB 018424 | INCB-018424 | INC424 Phosphate | Mitochondrial Autophagy | Ruxolitinib Phosphate | Ruxolitinib phosphate | INC 424 | INC-424 Phosphate | Inhibitor | INC 424 Phosphate | INCB-018424 Phosphate | INCB018424 Phosphate | Ruxolitinib (INCB-18424) Phosphate | JAK | INC-424 | Autophagy | Janus kinase

相关产品: AICAR phosphate | Tanespimycin | Valproic acid sodium salt | Sunitinib Malate | Ginsenoside Rb1 | Quinacrine dihydrochloride | Simvastatin | Resveratrol | Etoposide | Kaempferol

相关库: Drug Repurposing Compound Library | FDA-Approved Kinase Inhibitor Library | Anti-Cancer Drug Library | Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | Tyrosine Kinase Inhibitor Library | Anti-Cancer Approved Drug Library | Apoptosis Compound Library | EMA Approved Drug Library

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