INCB 018424 phosphate是一種有效的JAK1/2抑制劑，其IC50s分別為3.3 nM/2.8 nM，顯示出超過JAK 3 130倍的選擇性。

INCB018424有效并選擇性地抑制JAK2V617F介導(dǎo)的信號傳導(dǎo)和增殖。Ruxolitinib以186 nM的EC50抑制HEL細(xì)胞的生長。Ruxolitinib顯著增加Ba/F3-EpoR-JAK2V617F細(xì)胞系統(tǒng)中的凋亡，并抑制原發(fā)性MPN患者樣本中的造血祖細(xì)胞增殖[1]。

Ruxolitinib phosphate(180 mg/kg，口服)減少接種JAK2V617F表達(dá)細(xì)胞的小鼠的腫瘤負(fù)荷，而不引起貧血或淋巴細(xì)胞減少[1]。

產(chǎn)品性質(zhì)：

Cas No.:1092939-17-7

別名:魯索利替尼磷酸鹽,INCB018424 phosphate;INCB 018424 phosphate;INCB-018424 phosphate;Ruxolitinib

化學(xué)名: (3R)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]propanenitrile;phosphoric acid

Canonical SMILES:[HH].C1CCC(C1)C(CC#N)N2C=C(C=N2)C3=C4C=CNC4=NC=N3.OOP(=O)=O

分子式:C17H21N6O4P

分子量:404.36

溶解度:≥ 20.2 mg/mL in DMSO, ≥ 6.92 mg/mL in EtOH with ultrasonic and warming, ≥ 8.03 mg/mL in Water with ultrasonic and warming

儲存條件:Store at -20°C

注意事項(xiàng)：

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References:

[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.

[3]. de Bock CE, et al. HOXA9 Cooperates with Activated JAK/STAT Signaling to Drive Leukemia Development. Cancer Discov. 2018 May;8(5):616-631.