WP1066是AG490的類似物，是janus激酶2 (JAK2)的新型有效抑制劑，其抑制JAK2的磷酸化并降解JAK2蛋白，從而以劑量和時間依賴的方式阻斷JAK2下游信號轉導子和轉錄激活子(轉錄-3和轉錄-5)以及磷酸肌醇-3激酶途徑。初步研究的結果表明，WP1066抑制由抑制腫瘤血管生成的Caki-1腎癌細胞(RCC)產生的異種移植物腫瘤的生長，并在來自新診斷的AML患者的AML集落形成細胞以及AML細胞系OCIM2和K562中表現出抗增殖活性，這使其能夠治療RCC、急性髓性白血病(AML)和其他血液惡性腫瘤。

產品性質：

Cas No.：857064-38-1

別名：(2E)-3-(6-溴-2-吡啶基)-2-氰基-N-[(1S)-1-苯基乙基]-2-丙烯酰胺

化學名：(E)-3-(6-bromopyridin-2-yl)-2-cyano-N-[(1S)-1-phenylethyl]prop-2-enamide

Canonical SMILES：CC(C1=CC=CC=C1)NC(=O)C(=CC2=NC(=CC=C2)Br)C#N

分子式：C17H14BrN3O

分子量：356.22

溶解度：≥ 17.8 mg/mL in DMSO, ≥ 24.6 mg/mL in EtOH with ultrasonic and warming

儲存條件：Store at -20°C

注意事項：

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References:

[1].Srdan Verstovsek, Taghi Manshouri, Alfonso Quintas-Cardama, David Harris, Jorge Cortes, Francis J. Giles, Hagop Kantarjian, Waldemar Priebe, and Zeev Estrov. WP1066, a novel JAK2 inhibitor, suppresses proliferation and induces apoptosis in erythroid human cells carrying the JAK2 V617F mutation. Clin Cancer Res 2008; 14: 788-796

[2].Alessandra Ferrajoli, Stefan Faderl, Quin Van, Patricia Koch, David Harris, Zhiming Liu, Inbal Hazan-Halevy, Yongtao Wang, Hagop M. Kantarjian, Waldemar Priebe, and Zeev Estrov. WP1066 disrupts janus kinase-2 and induces caspase-dependent apoptosis in acute myelogenous leukemia cells. Cancer Res 2007; 67: 11291-11299

[3].A Horiguchi, T Asano, K Kuroda, A Sato, J Asakuma, K Ito, M Hayakawa, M Sumitomo and T Asano. STAT3 inhibitor WP1066 as a novel therapeutic agent for renal cell carcinoma. British Journal of Cancer 2010; 102: 1592-1599