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- 文献和实验
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- 保存条件：
4°C, sealed storage, away from moisture
- 英文名：
CYT387 sulfate salt
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
1056636-06-6
- 规格：
10 mM * 1 mL/5 mg/10 mg/50 mg/100 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥1142.0 |
|---|---|---|---|
| 规格： | 5 mg | 产品价格： | ￥850.0 |
| 规格： | 10 mg | 产品价格： | ￥1252.0 |
| 规格： | 50 mg | 产品价格： | ￥3464.0 |
| 规格： | 100 mg | 产品价格： | ￥5388.0 |
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Momelotinib sulfate
CAS No. : 1056636-06-6
MCE 国际站：Momelotinib sulfate
产品活性：Momelotinib sulfate (CYT387 sulfate salt) 是一种 ATP竞争性的 JAK1/JAK2 抑制剂，IC50 分别为 11 nM/18 nM，作用于JAK3时，IC50 为 155 nM。
研究领域：Epigenetics | Protein Tyrosine Kinase/RTK | JAK/STAT Signaling | Stem Cell/Wnt | Autophagy | Apoptosis
作用靶点：JAK | Autophagy | Apoptosis
In Vitro: Momelotinib sulfate (CYT387 sulfate salt) inhibits growth of Ba/F3-JAK2V617F and human erythroleukemia (HEL) cells (IC50=1.5 μM) or Ba/F3-MPLW515L cells (IC50=200 nM), but has considerably less activity against BCR-ABL harboring K562 cells (IC50=58 μM) and FLT3 mutation harboring MV4-11 cells (IC50=3 μM). Proliferation of parental Ba/F3 cells (Ba/F3-wt) stimulated with IL-3 is inhibited with an IC50 value of 1.4 μM, consistent with the established role of IL-3-dependent signaling in the parental cell line.
In Vivo: Momelotinib sulfate (CYT387 sulfate salt) at twice the dose used in disease model (50 and 100 mg/kg) has little to no effect on peripheral blood counts over a period of 8 weeks. Median plasma peak concentrations are 7.1 μM with the lower dose and 32.1μM with the higher dose, with a half-life of approximately 2 hours. Trough levels at 12 hours are 10nM for the 25 mg/kg and 900nM for the 50 mg/kg dose. At day 34 after transplantation, the mean white blood cell counts and hematocrit values of the entire cohort exceeded the normal range for Balb/c mice by more than 1 SD. At this point, 6 mice are sacrificed and subjected to autopsy. In the remaining animals, treatment is initiated with 25 mg/kg Momelotinib sulfate (CYT387 sulfate salt), 50 mg/kg Momelotinib sulfate (CYT387 sulfate salt), or vehicle, administered twice daily by oral gavage (12 mice per treatment group). A rapid drop of the white cell counts is apparent in both dose cohorts as early as 6 days after initiation of treatment and a decline of the hematocrit is apparent after 20 days. After oral dosing, Momelotinib sulfate (CYT387 sulfate salt) exhibits high plasma concentrations (Cmax= 40.4 μM; Tmax=4 h), with quantitative absolute oral bioavailability and an apparent half life of 2.4 h. The high oral bioavailability, can likely be partly ascribed to the low blood clearance of Momelotinib sulfate (CYT387 sulfate salt) (6.3 mL/min/kg) and therefore low susceptibility to hepatic first pass metabolism.
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文献和实验Metabolic Labeling with Sulfate
of proteins make it possible to determine where a protein normally resides or to follow its transport through the cell. One such modification is addition of sulfate either to tyrosine residues or to carbohydrate side chains. Labeling studies with [35 S
Ammonium Sulfate Binding Assay for Cells
1. Resuspend cells (vegetative or developed) in phosphate buffer at 1 x 10 8 /ml . 2. Add 50 ul cells to 50 ul 20 nM 3H-cAMP in 5-10 mM DTT (for background binding, add same amount of hot cAMP plus 10 uM cold cAMP) in 1.5 ml eppendorf tube
在哺乳动物真皮中发现的一种粘多糖。在真皮中，于成熟的胶原纤维丰富的层中，以蛋白多糖即以与蛋白质相结合的（蛋白硫酸皮肤素）形式而存在。因此胶原分子是按一定的空间排列集成，并由桥键组成纤维构造，而蛋白硫酸皮肤素具有重要作用。除皮肤以外，也可从大动脉、脐带、腱、心脏瓣膜、肝脏和半月瓣等分离出来，而在鼻软骨和骨端软骨中并不存在。化学构造如图所示是 L-艾杜糖醛酸和 N-乙酰半乳糖胺 -4-硫酸所形成的二糖单位的重复结构而为其主体，但糖醛酸的一部分为艾杜糖
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