CAS NO: | 700874-71-1 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
1 g | 电议 |
生物活性 | LY2109761 is an orally active, selectiveTGF-β receptortype I/IIinhibitor withKis of 38 nM and 300 nM, respectively. | ||||||||||||||||
IC50& Target | Ki: 38 nM (TβRI), 300 nM (TβRII) | ||||||||||||||||
体外研究 (In Vitro) | LY2109761 significantly inhibits the growth of L3.6pl/GLT soft agar colonies in a dose-dependent manner, and results in appr 33% inhibition at 2 μM and 73% inhibition at 20 μM. Targeting TβRI/II kinase activity with LY2109761 (5 μM) almost completely suppresses both the basal and TGF-β1-stimulated migration of L3.6pl/GLT cells[1]. LY2109761 induces a dose-dependent reduction in phosphorylation of Smad-2. HLE endogenous phosphorylation of Smad-2 is inhibited by LY2109761. LY2109761 blocks migration on different ECM proteins and invasion of both HLE and HLF through a 3-dimensional structure. LY2109761 increases E-cadherin mRNA expression after 24 hours and protein levels after 48 hours[2]. LY2109761 pretreatment reduces clonogenic survival in cell cultures of U87MG and T98 following radiation, resulting in an increase in the radiosensitivity with a DEF0.1 of 1.30 and 1.37, respectively[3]. | ||||||||||||||||
体内研究 (In Vivo) | LY2109761 (50 mg/kg, p.o.) greatly reduces the tumor volume and increases the median survival duration of the mice to 45.0 days. The mice treated with LY2109761 develop significantly fewer metastatic lesions and, in some of them, no metastatic lesion, as indicated by the GFP signal, can be identified in the abdomen[1]. LY2109761 enhances radiation-induced tumor growth delay in a U87MG subcutaneous xenograft tumor model in BALB/c nude mice. LY2109761 increases survival in an orthotopical CSLC glioblastoma model and enhanced antitumor activity of radiation[2]. | ||||||||||||||||
分子量 | 441.52 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C26H27N5O2 | ||||||||||||||||
CAS 号 | 700874-71-1 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : 25 mg/mL(56.62 mM;Need ultrasonic) 配制储备液
* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百
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