硫磺酰亚胺
| 中文名称 | 硫磺酰亚胺 |
|---|---|
| 中文同义词 | 抑胃酶氨酰U丙基亚胺;化合物 T16941;米哚妥林杂质5;硫磺酰亚胺;STAUPRIMIDE,抑制剂;化合物 STAUPRIMIDE |
| 英文名称 | StaupriMide |
| 英文同义词 | [9S-(9α,10β,11β,13α)]-N-(2,3,10,11,12,13-Hexahydro-10-methoxy-9-methyl-1,3-dioxo-9,13-epoxy-1H,9H-diindolo[1,2,3-gh:3',2',1'-lm]pyrrolo[3,4-j][1,7]benzodiazonin-11-yl)-N-methylbenzamide;N-Benzoyl-7-oxostaurosporine;benzaMide deriv.;Stauprimide;Stauprimide - CAS 154589-96-5 - Calbiochem;Benzamide, N-[(9S,10R,11R,13R)-2,3,10,11,12,13-hexahydro-10-methoxy-9-methyl-1,3-dioxo-9,13-epoxy-1H,9H-diindolo[1,2,3-gh:3',2',1'-lm]pyrrolo[3,4-j][1,7]benzodiazonin-11-yl]-N-methyl-;Stauprimide-d5;N-((5S,6R,7R,9S)-6-Methoxy-5-methyl-14,16-dioxo-6,7,8,9,15,16-hexahydro-5H,14H-17-oxa-4b,9a,15-triaza-5,9-methanodibenzo[b,h]cyclonona[jkl]cyclopenta[e]-as-indacen-7-yl)-N-methylbenzamide |
| CAS号 | 154589-96-5 |
| 分子式 | C35H28N4O5 |
| 分子量 | 584.62 |
| EINECS号 | |
| 相关类别 | 微生物代谢物;抗生素;Antibiotic;Chiral Reagents;Intermediates & Fine Chemicals;Pharmaceuticals;Isotope Labelled Compounds |
| Mol文件 | 154589-96-5.mol |
| 结构式 |  |
硫磺酰亚胺 性质
| 密度 | 1.52±0.1 g/cm3(Predicted) |
|---|---|
| 储存条件 | -20°C |
| 溶解度 | 二甲基亚砜：>20mg/mL |
| 酸度系数(pKa) | 9.51±0.70(Predicted) |
| 形态 | 黄色固体 |
| 颜色 | 白色至米色 |
| 稳定性 | 自购买之日起 2 年内保持稳定。 DMSO 溶液可在 -20°C 下保存长达 2 个月。 |
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. |
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. |
安全信息
| WGK Germany | 3 |
|---|---|
| 海关编码 | 2934999090 |