Ruxolitinib phosphate
作者：齐岳
发布时间：2023-09-12
09:13:52
点击数：
产品名称：Ruxolitinib phosphate
产品描述：
| 产品描述 | Ruxolitinib phosphate(INCB018424 phosphate) is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM, >130-fold selectivity for JAK1/2 versus JAK3. |
| 靶点活性 | JAK2:2.8 nM, JAK1:3.3 nM |
| 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]. |
| 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. |
| 别名 | INC 424 phosphate, INCB018424 phosphate, INC424, Ruxolitinib (INCB-18424) phosphate, 磷酸鲁索利替尼, INCB018424 |
| 化合物与蛋白结合的复合物 |
C-Src in complex with Ruxolitinib |
| 分子量 | 404.36 |
| 分子式 | C17H21N6O4P |
| CAS No. | 1092939-17-7 |
存储
| Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 70 mg/mL(173.1 mM)
H2O: 8 mg/mL(19.8 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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西安齐岳生物科技有限公司是集化学科研和定制与一体的高科技化学公司。业务范围包括化学试剂和产品的研发、生产、销售等。涉及产品为通用试剂的分销、非通用试剂的定制与研发，涵盖生物科技、化学品、中间体和化工材料等领域。
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