中文名 | WYE-354 |
英文名 | WYE-354 |
别名 | 化合物AOB2796 MTOR抑制剂(WYE-354) 4-(6-(4-((甲氧羰基)氨基)苯基)-4-吗啉基-1H-吡唑并[3,4-D]嘧啶-1-基)哌啶-1-甲酸甲酯 4-[6-[4-[(甲氧羰基)氨基]苯基]-4-(4-吗啉基)-1H-吡唑并[3,4-D]嘧啶-1-基]-1-哌啶羧酸甲酯 |
英文别名 | CS-441 WYE-354 WYE354 WYE 354 WYE-354 (Degrasyn) Methyl 4-(6-(4-(methoxycarbonylamino)phenyl)-4-morpholino-1H-pyrazolo[3,4-d]pyrimidin-1-yl)pip methyl 4-[6-[4-(methoxycarbonylamino)phenyl]-4-morpholin-4-ylpyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carboxylate 4-[6-[4-[(Methoxycarbonyl)amino]phenyl]-4-(4-morpholinyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]-1-piperidinecarboxylic acid methyl ester 1-Piperidinecarboxylic acid, 4-[6-[4-[(methoxycarbonyl)amino]phenyl]-4-(4-morpholinyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]-, methyl ester |
CAS | 1062169-56-5 |
化学式 | C24H29N7O5 |
分子量 | 495.53 |
密度 | 1.46 |
酸度系数 | 13.42±0.70(Predicted) |
存储条件 | Sealed in dry,Store in freezer, under -20°C |
体外研究 | In the DELFIA measuring His6-S6K1 T389 phosphorylation, WYE-354 inhibits recombinant mTOR enzyme with an IC 50 of 5 nM. Cell viability is analyzed by MTS assay. G-415 and TGBC-2TKB cell lines are treated with increasing concentrations of WYE-354 (0.1, 1, 5 and 10 μM) for 24, 48, and 72 hours. WYE-354 significantly reduces cell viability starting at a 1 μM concentration after a 24 hours exposure, in both studied cell lines (P<0.001). A decrease in cell viability is not observed at a dose of 100 nM, except for the TGBC-2TKB cell line after 72 hours of treatment. |
体内研究 | The effect of Rapamycin and WYE-354 on tumor growth is evaluated in xenograft GBC tumor models. 2×10 6 or 5×10 6 cells of G-415 or TGBC2TKB, respectively, are xenotransplanted into NOD-SCID mice subcutaneously. When tumors reach an average volume of 100 mm 3 , the mice are treated either with Rapamycin or WYE354. Rapamycin is administered i.p. at a concentration of 10 mg/kg, daily for 5 days per week for 3 weeks, while WYE-354 is administrated at a daily i.p. dose of 50 mg/kg for 5 days. Mice are sacrificed 30 days after the initiation of the treatments and an autopsy is performed that include removal of the entire tumor area. Mice treated with WYE-354 exhibit 68.6% and 52.4% reduction in average tumor size (P<0.01; P<0.01), as well as 82.9% and 45.5% (P<0.01; ns) reduction in tumor weight, respectively. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.018 ml | 10.09 ml | 20.18 ml |
5 mM | 0.404 ml | 2.018 ml | 4.036 ml |
10 mM | 0.202 ml | 1.009 ml | 2.018 ml |
5 mM | 0.04 ml | 0.202 ml | 0.404 ml |
微信搜索化工百科或扫描下方二维码,添加化工百科小程序,随时随地查信息!