Ruxolitinib phosphate|1092939-17-7|(INCB018424 phosphate)-陌孚医药/Medlife

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Ruxolitinib phosphate (Synonyms: INCB018424 phosphate)

目录号: PL07367 纯度: ≥99%

CAS No. :1092939-17-7

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中文名称	Ruxolitinib phosphate
中文别名	鲁索替尼磷酸盐;β-环戊基-4-(7h-吡咯并[2,3-d]嘧啶-4-基)-(βr)-1H-吡唑-1-丙腈磷酸盐;磷酸鲁索替尼;(betaR)-beta-环戊基-4-(7H-吡咯并[2,3-d]嘧啶-4-基)-1H-吡唑-1-丙腈磷酸盐;8-溴茶碱;Ruxolitinib磷酸盐;卢索替尼磷酸盐;鲁索利替尼;鲁索利替尼磷酸盐;磷酸鲁索利替尼
英文名称	Ruxolitinib phosphate
英文别名	INCB 018424;(betaR)-beta-Cyclopentyl-4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazole-1-propanenitrile phosphate;Ruxolitinib Phosphate;(R)-3-(4-(7H-Pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile phosphate;[14C]-Ruxolitinib phosphate;betaR)-beta-Cyclopentyl-4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazole-1-propanenitrile phosphate;Ruxolitinib Phosphat;β-cyclopentyl-4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-(βR)-1H-Pyrazole-1-propanenitrile phosphate;(3R)-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]propionitrile phosphate;INCB018424 phosphate;INCB-018424 phosphate;Ruxolitinib;Ruxolitinib phosphate
Cas No.	1092939-17-7
分子式	C₁₇H₁₈N₆^.H₃Po₄
分子量	404.14
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情

Ruxolitinib phosphate (INCB018424 phosphate) 是一种有效的 JAK1/2 抑制剂， IC₅₀ 分别为3.3 nM/2.8 nM，比JAK3选择性高130倍。

生物活性

Ruxolitinib phosphate (INCB018424 phosphate) is a potent JAK1/2 inhibitor with IC 50 s of 3.3 nM/2.8 nM, respectively, showing more than 130-fold selectivity over JAK3.

性状

Solid

IC50 & Target[1][2]

JAK2 2.8 nM (IC50) JAK1 3.3 nM (IC50

体外研究(In Vitro)

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, and inhibits hematopoietic progenitor cell proliferation in primary MPN patient samples. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Ruxolitinib (180 mg/kg, p.o.) reduces the tumor burden of mice inoculated with JAK2V617F-expressing cells without causing anemia or lymphopenia. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ClinicalTrial

参考文献

[1]. Quintas-Cardama A, et al. Preclinical characterization of the selective JAK1/2 inhibitor INCB018424: therapeutic implications for the treatment of myeloproliferative neoplasms. Blood, 2010, 115(15), 3109-3117.
[2]. Fleischman AG, et al. The CSF3R T618I mutation causes a lethal neutrophilic neoplasia in mice that is responsive to therapeutic JAK inhibition. Blood. 2013 Nov 21;122(22):3628-31.

溶解度数据	In Vitro: DMSO : ≥ 31 mg/mL (76.66 mM)H₂O : 10 mg/mL (24.73 mM; Need ultrasonic)

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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