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
- 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.
- 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。
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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.
- 更新日期:2024/11/08
- 产品编号:HY-N6747
- 产品名称:Stauprimide
- CAS编号:
- 包装:1 mg
- 价格:2200元
- 更新日期:2024/08/19
- 产品编号:HY-N6747
- 产品名称:Stauprimide
- CAS编号:
- 包装:5 mg
- 价格:7000元
- 公司名称:Novachemistry
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