154589-96-5
154589-96-5 結(jié)構(gòu)式
基本信息
Stauprimide-d5
benzaMide deriv.
N-Benzoyl-7-oxostaurosporine
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-
[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
物理化學(xué)性質(zhì)
常見問題列表
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. |