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首页-小分子抑制剂&激动剂-JAK/STAT Signaling-JAK-Ruxolitinib sulfate
Ruxolitinib sulfate

Chemical Structure : Ruxolitinib sulfate

CAS No.: 1092939-16-6

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Ruxolitinib sulfate (INCB-018424 sulfate, INCB18424 sulfate)

货号: PC-45875Not For Human Use, Lab Use Only.

Ruxolitinib sulfate (INCB-018424 sulfate, INCB18424 sulfate) potent, selective, orally active JAK1/JAK2 inhibitor with IC50 of 3.3/2.8 nM, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Ruxolitinib sulfate (INCB-018424 sulfate, INCB18424 sulfate)  potent, selective, orally active JAK1/JAK2 inhibitor with IC50 of 3.3/2.8 nM, respectively.
Ruxolitinib displays modest selectivity against Tyk2 (6-fold) and marked selectivity (>130-fold) against JAK3.
Ruxolitinib inhibits IL-6 signaling (IC50=281 nM), and proliferation of JAK2V617F(+) Ba/F3 cells (IC50=127 nM).
Ruxolitinib suppresses erythroid progenitor colony formation from JAK2V617F(+) polycythemia vera patients (IC50=67 nM) in primary cultures.
Ruxolitinib markedly reduces level of inflammatory cytokines, and preferentially eliminates neoplastic cells in a mouse model of JAK2V617F(+) MPN.

物理化学性质&存储条件

分子量 404.4435
分子式 C17H20N6O4S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

1H-Pyrazole-1-propanenitrile, .beta.-cyclopentyl-4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-, (.beta.R)-, sulfate (1:1)

参考文献

1. Quintás-Cardama A, et al. Blood. 2010 Apr 15;115(15):3109-17.

2. Fridman JS, et al. J Immunol. 2010 May 1;184(9):5298-307.

3. Verstovsek S, et al. N Engl J Med. 2010 Sep 16;363(12):1117-27.

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