| 货号 | 规格 | 价格 | 上海 | 北京 | 珠海 | 重庆 | 武汉 | 购买数量 |
|---|---|---|---|---|---|---|---|---|
Y56802-5mg促销 |
≥98% | ￥280.00 ￥252.00 |
10 | - | - | - | - |
|
Y56802-10mg促销 |
≥98% | ￥452.00 ￥406.00 |
7 | - | - | - | - |
|
Y56802-25mg促销 |
≥98% | ￥1040.00 ￥936.00 |
5 | - | - | - | - |
|
Y56802-50mg促销 |
≥98% | ￥2300.00 ￥2070.00 |
2 | - | - | - | - |
|
Y56802-100mg促销 |
≥98% | ￥4040.00 ￥3640.00 |
1 | - | - | - | - |
|
| 产品描述： | RPI-1 is a specific, orally available 2-indolinone Ret tyrosine kinase inhibitor. RPI-1 inhibits proliferation, Ret tyrosine phosphorylation, Ret protein expression, and the activation of PLCgamma, ERKs and AKT in human medullary thyroid carcinoma TT cells. Antitumor activity | ||||||||||||||||||||
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| 靶点： | RET;Phospholipase; c-Met/HGFR; c-RET | ||||||||||||||||||||
| 体外研究： | TPC-1 cells are sensitive to the growth inhibitory effect of RPI-1 with an IC50 of 5.1 μM, following 72 hours of treatment. RPI-1 (7.5-60 µM) inhibits Ret/Ptc1 autophosphorylation in TPC-1 cells. RPI-1 inhibitory effects in the TPC-1 cell culture conditions lead to inhibition of pathways involving JNK2 and AKT. The RPI-1 IC50 value for cell proliferation is 3.6 µM in NIH3T3 cells expressing the Ret mutant compared with 16 µM in non-transfected NIH3T3 cells, and that for colony formation in soft agar was 2.4 µM and 26 µM in RET mutant-transfected and H-RAS-transfected NIH3T3 cells, respectively. In NIH3T3 cells expressing the Ret mutant, Ret protein and tyrosine phosphorylation were undetectable after 24 hours of RPI-1 treatment. In TT cells, RPI-1 inhibits proliferation, Ret tyrosine phosphorylation, Ret protein expression, and the activation of PLCgamma, ERKs and AKT. |
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| 体内研究： | RPI-1 (50, 100 mg/kg; p.o.; twice a day for 10 days) inhibits the tumor growth of TT xenografts by 81%. Animal Model: 8- to 11-week-old female athymic nude CD-1 mice (bearing TT cells) Dosage: 50, 100 mg/kg Administration: P.o.; twice a day for 10 days Result: A dose-dependent effect on tumor growth was observed, with a dose of 2*50 mg/kg/day resulting in less tumor weight inhibition than the 2*100mg/kg/day dose after 10 days of treatment. | ||||||||||||||||||||
| 参考文献： | 1. Lanzi C, et al. Inactivation of Ret/Ptc1 oncoprotein and inhibition of papillary thyroid carcinoma cell proliferation by indolinone RPI-1. Cell Mol Life Sci. 2003;60(7):1449-1459. 2. Cuccuru G, et al. Cellular effects and antitumor activity of RET inhibitor RPI-1 on MEN2A-associated medullary thyroid carcinoma. J Natl Cancer Inst. 2004;96(13):1006-1014. | ||||||||||||||||||||
| 溶解性： | Soluble in DMSO | ||||||||||||||||||||
| 保存条件： | -20℃ | ||||||||||||||||||||
| 配置溶液浓度参考： |
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| 注意： | 部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
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