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Stauprimide
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Stauprimide图片
CAS NO:154589-96-5
包装与价格:
包装价格(元)
500ug电议
1mg电议
5mg电议

产品介绍
Stauprimide 是一种星形孢菌素类似物,可促进胚胎干细胞 (ESC) 分化。 Stauprimide 是一种非广谱抑制剂,可与 MYC 转录因子 NME2 结合并阻断其在 ESC 中的核定位,从而导致 MYC 转录下调。
Cas No.154589-96-5
化学名N-((5S,6S,7R,9S)-6-methoxy-5-methyl-14,16-dioxo-5,6,7,8,9,14,15,16-octahydro-17-oxa-4b,9a,15-triaza-5,9-methanodibenzo[b,h]cyclonona[jkl]cyclopenta[e]-as-indacen-7-yl)-N-methylbenzamide
Canonical SMILESO=C(C1=C2C3=C(C4=C15)N(C6=CC=CC=C46)[C@H]7O[C@]([C@H]([C@@H](C7)N(C(C8=CC=CC=C8)=O)C)OC)(C)N3C9=CC=CC=C29)NC5=O
分子式C35H28N4O5
分子量584.62
溶解度DMF: 25 mg/ml,DMF:PBS(pH7.2) (1:2): 0.3 mg/ml,DMSO: 10 mg/ml,Ethanol: 0.2 mg/ml
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Stauprimide is a staurosporine analog that promotes embryonic stem cell (ESC) differentiation. Stauprimide is a non-broad spectrum inhibitor that binds to the MYC transcription factor NME2 and blocks its nuclear localization in ESCs, which results in down-regulation of MYC transcription[1].

Stauprimide (10 μM; 6 hours) suppresses MYC transcription in the majority of cell lines tested with an EC50 range of 30 nM-8 μM, and decreases MYC levels between 15% to over 90%[1]. Stauprimide (2-8 μM; 24-72 hours) down-regulates MYC leads to the inhibition of cell proliferation in vitro with an IC50 of 780 nM in RXF 393 cells[1]. Stauprimide (5 μM; 3 hours) suppresses MYC Transcription by decreasing NME2 Nuclear Translocation[1]. Stauprimide (4-10 μM; 6 hours) acts with different EC50s and with different degrees of maximal MYC mRNA down-regulation in different cell lines[1].

Stauprimide (oral administration; 50 mg/kg; once daily; 30 days, 55 days) blocks tumor growth, reduces MYC protein levels in xenograft mouse with RXF 393 or CAKI-1 cells and inhibits MYC transcription in the RXF 393 tumor[1].

References:
[1]. Bouvard C, et al. Small molecule selectively suppresses MYC transcription in cancer cells. Proc Natl Acad Sci USA. 2017 Mar 28;114(13):3497-3502.