生物活性

WP1066, an analogue of AG490, is a novel and potent inhibitor of janus kinase 2 (JAK2), which inhibits the phosphorylation of JAK2 and degrades JAK2 protein consequently blocking JAK2’s downstream signal transducer and activator of transcription (transcription-3 and transcription-5) as well as phosphoinositide-3-kinase pathways in a dose- and time-dependent manner. Results of preliminary studies suggest that WP1066 inhibits the growth of xenograft tumors generated from Caki-1 renal carcinoma cells (RCC) suppressing tumor angiogenesis and exhibits antiproliferative activity in AML colony-forming cells from newly diagnosed AML patients as well as in AML cell lines OCIM2 and K562, which potentiates it to treat RCC, acute myeloid leukemia (AML) and other hematologic maglignancies.

体外研究

体内研究

DMSO:聚乙二醇 300 (20:80)

激酶实验

细胞实验

动物实验

40 mg/kg 一天一次口服17天

不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。

参考文献

[1] Verstovsek S, et al. Clin Cancer Res, 2008, (3), 788-796.
[2] Hussain, S.F., et al. 2007. Cancer Res. 67: 9630-9636.
[3] Ferrajoli, A., et al. 2007. Cancer Res. 67: 11291-11299.
[4] Iwamaru, A., et al. 2007. Oncogene. 26: 2435-2444.
[5] McGaffin, K.R., et al. 2009. Cardiovasc. Res. 83: 313-324.

体内溶解度

Clinical Trial Information ( data from http://clinicaltrials.gov )

注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。

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