硫磺酰亚胺

生物活性体外研究体内研究硫磺酰亚胺试剂级价格

硫磺酰亚胺

CAS号:154589-96-5
英文名:StaupriMide
中文名:硫磺酰亚胺
CBNumber:CB32518818
分子式:C35H28N4O5
分子量:584.62
MOL File:154589-96-5.mol

硫磺酰亚胺化学性质

密度 :1.52±0.1 g/cm3(Predicted)
储存条件 :-20°C
溶解度 :DMSO: >20mg/mL
酸度系数(pKa) :9.51±0.70(Predicted)
形态 :Yellow solid
颜色 :white to beige
稳定性 :Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months.

安全信息

WGK Germany :3
海关编码 :2934999090

硫磺酰亚胺性质、用途与生产工艺

生物活性 Stauprimide 是一种促进胚胎干细胞 (ESC) 分化的星形孢菌素类似物。Stauprimide 与 MYC 转录因子 NME2 结合并阻断其在 ESC 中的核定位，导致 MYC 转录的下调, 是一种非广谱抑制剂。

体外研究

Stauprimide (10 μM; 6 hours) suppresses MYC transcription in the majority of cell lines tested with an EC ₅₀ range of 30 nM-8 μM, and decreases MYC levels between 15% to over 90%. Stauprimide (2-8 μM; 24-72 hours) down-regulates MYC leads to the inhibition of cell proliferation in vitro with an IC ₅₀ of 780 nM in RXF 393 cells. Stauprimide (5 μM; 3 hours) suppresses MYC Transcription by decreasing NME2 Nuclear Translocation. Stauprimide (4-10 μM; 6 hours) acts with different EC ₅₀ s and with different degrees of maximal MYC mRNA down-regulation in different cell lines.

Cell Proliferation Assay

Cell Line:	Renal cancer cell line RXF 393 cells
Concentration:	2 μM, 4 μM, 8 μM
Incubation Time:	24 hours, 48 hours, 72 hours
Result:	Inhibited cell proliferation at concentrations of 2-8 μM.

Western Blot Analysis

Cell Line:	Renal cancer cell line RXF 393 cells and CAKI-1 cells
Concentration:	5 μM
Incubation Time:	3 hours
Result:	Decreased nuclear localized NME2.

RT-PCR

Cell Line:	CA46 cells; Ramos cells; RXF393 cells; TK10 cells; KG1A cells; CAKI-1 cells
Concentration:	4μM, 6μM, 8μM, 10μM
Incubation Time:	6 hours
Result:	Suppressed MYC transcription in KG1A cells with an EC ₅₀ of 400±50 nM and a suppression of 90%; CA46 cells were resistant to stauprimide.

体内研究

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.

Animal Model:	Xenograft tumor models with RXF 393 and CAKI-1 cells in NOD/SCID mice
Dosage:	50 mg/kg
Administration:	Oral administration; 50 mg/kg; once daily; 30 days, 55 days
Result:	Blocked tumor growth in mice injected with either RXF 393 or CAKI-1 cells during the dosing periods.